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Drug delivery systems: An updated review
Gaurav Tiwari, Ruchi Tiwari, Birendra Sriwastawa, L Bhati, S Pandey, P Pandey, Saurabh K Bannerjee
January-March 2012, 2(1):2-11
DOI:10.4103/2230-973X.96920  PMID:23071954
Drug delivery is the method or process of administering a pharmaceutical compound to achieve a therapeutic effect in humans or animals. For the treatment of human diseases, nasal and pulmonary routes of drug delivery are gaining increasing importance. These routes provide promising alternatives to parenteral drug delivery particularly for peptide and protein therapeutics. For this purpose, several drug delivery systems have been formulated and are being investigated for nasal and pulmonary delivery. These include liposomes, proliposomes, microspheres, gels, prodrugs, cyclodextrins, among others. Nanoparticles composed of biodegradable polymers show assurance in fulfilling the stringent requirements placed on these delivery systems, such as ability to be transferred into an aerosol, stability against forces generated during aerosolization, biocompatibility, targeting of specific sites or cell populations in the lung, release of the drug in a predetermined manner, and degradation within an acceptable period of time.
  17,845 3,904 131
Formulation development and in vitro evaluation of gastroretentive hollow microspheres of famotidine
Mayur A Chordiya, Hemant H Gangurde, K Senthilkumaran, Lokesh P Kothari
April-June 2011, 1(2):105-111
DOI:10.4103/2230-973X.82423  PMID:23071929
Background: The main aim of this study was to develop a gastroretentive, multiple-unit floating drug delivery system for a drug which is poorly absorbed from the lower gastrointestinal tract. Such a dosage form may provide an extended retention of drug in the upper gastrointestinal tract resulting in enhanced absorption and improved bioavailability. Materials and Methods: Microspheres were prepared by the emulsion solvent diffusion method. Four different ratios (1:1, 1:2, 1:3, and 1:4) from each polymer, i.e., Eudragit RL 100 (E1-E4) and cellulose acetate (C1-C4) were prepared. Results: Hollow microspheres were characterized by particle size using optical microscopy. The in vitro release data obtained for the formulations E1-E4 and C1-C4 showed good entrapment efficiency, good percentage buoyancy, and prolonged drug release. The in vitro drug release showed the highest regression coefficient values for Higuchi's model, indicating diffusion to be the predominant mechanism of drug release. The surface and cross-sectional morphology of the formulations E1-A and C1-A were determined using scanning electron microscopy. Conclusions: Thus, prepared floating hollow microspheres of famotidine may prove to be potential candidates for the multiple-unit drug delivery device adaptable for any intragastric condition.
  13,825 1,026 1
Formulation strategies for drug delivery of tacrolimus: An overview
Pranav Patel, Hitesh Patel, Shital Panchal, Tejal Mehta
October-December 2012, 2(4):169-175
DOI:10.4103/2230-973X.106981  PMID:23580932
Tacrolimus (FK 506) is a potent macrolide lactone immunosuppressive agent used for prophylaxis of organ rejection after transplantation and graft-versus-host disease after bone marrow transplantation in patients. Moreover, tacrolimus is a drug of choice in the treatment of atopic dermatitis for decreasing side effects associated with the use of topical corticosteroids. In spite of its success in ensuring graft survival, therapeutic use of tacrolimus is complicated due to its narrow therapeutic index (between 5 and 15 ng/ml). Tacrolimus has a large inter-/intra-patient variability in pharmacokinetics profile and a poor oral bioavailability because of its poor solubility, P-gp efflux, marked pre-systemic metabolism by CYP3A in the enterocytes and liver first pass effect. Several formulation approaches such as oily solution, solid dispersions, complexation with cyclodextrins, liposomes etc., have been investigated to improve oral delivery of FK 506. In this review, we have discussed various formulation approaches that have been undertaken by various researchers to solve the problems related to the drug delivery of tacrolimus.
  6,579 6,042 23
Recent trends in vaccine delivery systems: A review
CH Saroja, PK Lakshmi, Shyamala Bhaskaran
April-June 2011, 1(2):64-74
DOI:10.4103/2230-973X.82384  PMID:23071924
Vaccines are the preparations given to patients to evoke immune responses leading to the production of antibodies (humoral) or cell-mediated responses that will combat infectious agents or noninfectious conditions such as malignancies. Alarming safety profile of live vaccines, weak immunogenicity of sub-unit vaccines and immunization, failure due to poor patient compliance to booster doses which should potentiate prime doses are few strong reasons, which necessitated the development of new generation of prophylactic and therapeutic vaccines to promote effective immunization. Attempts are being made to deliver vaccines through carriers as they control the spatial and temporal presentation of antigens to immune system thus leading to their sustained release and targeting. Hence, lower doses of weak immunogens can be effectively directed to stimulate immune responses and eliminate the need for the administration of prime and booster doses as a part of conventional vaccination regimen. This paper reviews carrier systems such as liposomes, microspheres, nanoparticles, dendrimers, micellar systems, ISCOMs, plant-derived viruses which are now being investigated and developed as vaccine delivery systems. This paper also describes various aspects of "needle-free technologies" used to administer the vaccine delivery systems through different routes into the human body.
  10,950 1,544 23
Orally dissolving strips: A new approach to oral drug delivery system
Rajni Bala, Pravin Pawar, Sushil Khanna, Sandeep Arora
April-June 2013, 3(2):67-76
DOI:10.4103/2230-973X.114897  PMID:24015378
Recently, fast dissolving films are gaining interest as an alternative of fast dissolving tablets. The films are designed to dissolve upon contact with a wet surface, such as the tongue, within a few seconds, meaning the consumer can take the product without need for additional liquid. This convenience provides both a marketing advantage and increased patient compliance. As the drug is directly absorbed into systemic circulation, degradation in gastrointestinal tract and first pass effect can be avoided. These points make this formulation most popular and acceptable among pediatric and geriatric patients and patients with fear of choking. Over-the-counter films for pain management and motion sickness are commercialized in the US markets. Many companies are utilizing transdermal drug delivery technology to develop thin film formats. In the present review, recent advancements regarding fast dissolving buccal film formulation and their evaluation parameters are compiled.
  9,439 2,079 25
Prefilled syringes: An innovation in parenteral packaging
Sagar Makwana, Biswajit Basu, Yogita Makasana, Abhay Dharamsi
October-December 2011, 1(4):200-206
DOI:10.4103/2230-973X.93004  PMID:23071944
Parenteral administration of pharmaceutical products is one of the most popular methods used to produce quick onset of action and also 100% bioavailability. Main problem occurs with the parenteral drug delivery is lack of convenience, affordability, accuracy, sterility, safety etc. Such drawbacks with this delivery system makes it less preferable. Hence, all the disadvantages of these systems can be easily overcome by use of prefilled syringes. The objective of this review article is to provide information regarding prefilled syringes; it's method of preparation, direction to use, advantages, its future scope, and development.
  9,263 1,806 15
Formulation and evaluation of fast dissolving films of levocitirizine di hydrochloride
Prabhakara Prabhu, Ravi Malli, Marina Koland, K Vijaynarayana, Ullas D'Souza, NM Harish, CS Shastry, RN Charyulu
April-June 2011, 1(2):99-104
DOI:10.4103/2230-973X.82417  PMID:23071928
Introduction: Levocetirizine dihydrochloride is an orally active, third-generation non-sedative antihistamine used in the symptomatic relief of seasonal and perennial allergic rhinitis. The present work aimed at preparing quick release films of levocetirizine with the purpose of developing a dosage form for a very quick onset of action, which is beneficial in managing severe conditions of allergies, aiding in the enhancement of bioavailability, and is very convenient for administration, without the problem of swallowing and using water. Materials and Methods: The films of levocetirizine dihydrochloride were prepared by using polymers such as hydroxypropyl methylcellulose (HPMC) and polyvinyl alcohol (PVA), as either single polymer or in combination of two, by a solvent casting method. They were evaluated for physical characteristics such as uniformity of weight, thickness, folding endurance, drug content uniformity, surface pH, percentage elongation, and tensile strength, and gave satisfactory results. The formulations were subjected to disintegration, in vitro drug release tests, and in vivo studies on rats. Results: A marked increase in the dissolution rate was exhibited by fast-dissolving films of levocetirizine dihydrochloride containing HPMC as a polymer, when compared to conventional tablets. The haloperidol-induced catalepsy, milk-induced leukocytosis, and nasal provocation in vivo studies in rats proved that the fast-dissolving films of levocetirizine dihydrochloride produced a faster onset of action compared to the conventional tablets. Conclusions: Fast dissolving films of levocetirizine dihydrochloride can be considered suitable for clinical use in the treatment of allergic rhinitis and other conditions of allergies, where a quicker onset of action for a dosage form is desirable along with the convenience of administration.
  8,799 1,731 14
Formulation and evaluation of bucco-adhesive tablets of sumatriptan succinate
R Indira Prasanna, P Anitha, C Madhusudhana Chetty
July-September 2011, 1(3):182-191
DOI:10.4103/2230-973X.85971  PMID:23071941
Background: A novel aspiration in treatment of migraine, to provide greater therapeutic effect, overcome the side effects by complex therapeutic regimen and to improve patient compliance upon administering bucco-adhesive tablet formulations of sumatriptan succinate which have not been tested literally. Materials and Methods: This study was designed to develop a bucco-adhesive tablet containing sumatriptan succinate using blends of different bio-adhesive polymeric combinations such as hydroxy propyl methyl cellulose K4M, sodium carboxy methyl cellulose, and Carbopol 934P with a backing layer of ethyl cellulose by a direct compression technique. Tablets were subjected to physico-chemical parameters, swelling index, surface pH, ex vivo bioadhesive force, in vitro drug release, ex vivo drug permeation, and stability in saliva. Results: Good results were obtained in all the evaluated parameters. The drug release of all formulation follows zero-order kinetics by a diffusion mechanism type. Stability studies in human saliva, ex vivo buccal permeation studies by using sheep and porcine buccal mucosa were carried out for the optimized formulation (S4 CP:HPMC 3:1). Conclusion: The developed buccal drug delivery system containing sumatriptan succinate might be the alternative routes available to bypass the first pass metabolism and might be a milestone in the therapy of migraine and among all formulations S4 shows good controlled release results correlated with ex vivo permeation studies.
  8,475 930 6
Preparation and characterization of albumin nanoparticles encapsulating curcumin intended for the treatment of breast cancer
AV Jithan, K Madhavi, M Madhavi, K Prabhakar
April-June 2011, 1(2):119-125
DOI:10.4103/2230-973X.82432  PMID:23071931
Introduction: For the real-time clinical utilization of curcumin (an ayurvedic natural product) to treat breast cancer, its dissolution, rate limited solubility, poor tissue absorption, and extensive in vivo metabolism that leads to its poor systemic bioavailability should be overcome. A polymer-based nanoparticle formulation using bovine serum albumin can increase its aqueous solubility and can achieve protected, sustained, and targeted therapy in breast cancer. Materials and Methods: Desolvation technique was optimized for the preparation of albumin nanoparticles. Particle size, drug release, encapsulation efficiency, drug polymer interaction were the in vitro properties that were determined. Cell culture studies, in vivo pharmacokinetics in rats were used for biological characterization of the formulation. Results: The formulations were successfully prepared using 1:1, 1:2, 1:3, 1:4 drug: polymer ratios and the percent entrapment was found to be 74.76%, 91.01%, 85.36%, 86.42%, respectively, and particle size determined by zetasizer was found to be 225.1, 223.5, 226.3, 228.7 nm, respectively, and in vitro release was sustained for at least one month with drug release of 75.74%, 65.97%, 64.42%, 54%, respectively. The dissolution rate and aqueous solubility of curcumin was enhanced with this formulation. Fourier transform infrared spectroscopy (FTIR) studies demonstrated that the drug was not changed in the formulation during the fabrication process. The proliferation assays in MDA-MB-231 tumor cell lines indicated more effectiveness of the formulation compared to its solution form. In rats, albumin nanoparticles sustained drug release, demonstrated more bioavailability, improved pharmacokinetic properties, and enhanced tissue targetability of the drug. Conclusions: An effective curcumin-albumin nanoparticle formulation was successfully developed using a desolvation technique.
  7,436 1,689 33
Chemical stability of tramadol hydrochloride injection admixed with selected pain drugs
V Di Stefano, R Pitonzo, S Bavetta, P Polidori, MG Sidoti
January-March 2011, 1(1):48-52
DOI:10.4103/2230-973X.76729  PMID:23071920
Background: Tramadol hydrochloride (HCl) and ketorolac tromethamine are analgesic drugs, which are commonly used in combination in postoperative pain management. According to some studies, metoclopramide and magnesium sulfate (MgSO 4 ) as adjuvant agents can improve analgesia and decrease the need for other pain drugs. Materials and Methods: The chemical stability of tramadol HCl combined with ketorolac tromethamine and metoclopramide HCl has been studied using a stability-indicating high-performance liquid chromatographic assay method. Calibration curves were produced using linear regression of the peak area against concentration of each drug, with an r 2 value ≥ 0.96. Our aim was to investigate the stability of admixture solution of tramadol HCl combined with ketorolac tromethamine and metoclopramide HCl for 48 h (25ºC) and 5 days (5ºC), with MgSO 4 , which has never been assessed. Results: Data obtained for admixtures prepared and stored at temperatures of 25ºC and 5ºC, show that all drugs have reached at least 98% of the initial concentration. Conclusions: For the purpose of pre-preparing drug admixtures to use with confidence, tramadol HCl infusions may be prepared in advance and then thawed before use in clinical units. On the basis of our results, the intravenous mixture of tramadol (7.69 mg/mL), metoclopramide (0.19 mg/mL), ketorolac (1.15 mg/mL), and magnesium sulfate (77 mg/mL) may be considered for a possible commercial formulation.
  8,414 570 2
Study on sustained-release metformin hydrochloride from matrix tablet: Influence of hydrophilic polymers and in vitro evaluation
Kamlesh J Wadher, Rajendra B Kakde, Milind J Umekar
July-September 2011, 1(3):157-163
DOI:10.4103/2230-973X.85966  PMID:23071938
The overall objective of the present work was to develop an oral sustained-release (SR) metformin tablet prepared by the direct compression method, using hydrophilic hydroxylpropylmethylcellulose (HPMC) and Guar gum polymer alone and in combination at different concentrations. Metformin hydrochloride (HCl), a biguanide, has a relatively short plasma half-life and low absolute bioavailability. All the batches were evaluated for thickness, weight variation, hardness and drug content uniformity and in vitro drug release. Mean dissolution time is used to characterize the drug release rate from a dosage form, and indicates the drug release-retarding efficiency of the polymer. The hydrophilic matrix of HPMC alone could not control the Metformin release effectively for 12 h whereas when combined with Guar gum, it could slow down the release of drug and, thus, can be successfully employed for formulating SR matrix tablets. Fitting the data to the Korsmeyer equation indicated that diffusion along with erosion could be the mechanism of drug release. Similarity factor ƒ2 values suggest that the test and reference profiles are identical.
  7,644 1,007 4
Quality risk management of top spray fluidized bed process for antihypertensive drug formulation with control strategy engendered by Box-behnken experimental design space
Amit Mukharya, Paresh U Patel, Dinesh Shenoy, Shivang Chaudhary
January-March 2013, 3(1):15-28
DOI:10.4103/2230-973X.108960  PMID:23799202
Introduction: Lacidipine (LCDP) is a very low soluble and highly biovariable calcium channel blocker used in the treatment of hypertension. To increase its apparent solubility and to reduce its biovariability, solid dispersion fluid bed processing technology was explored, as it produces highly dispersible granules with a characteristic porous structure that enhances dispersibility, wettability, blend uniformity (by dissolving and spraying a solution of actives), flow ability and compressibility of granules for tableting and reducing variability by uniform drug-binder solution distribution on carrier molecules. Materials and Methods: Main object of this quality risk management (QRM) study is to provide a sophisticated "robust and rugged" Fluidized Bed Process (FBP) for the preparation of LCDP tablets with desired quality (stability) and performance (dissolution) by quality by design (QbD) concept. Results and Conclusion: This study is principally focusing on thorough mechanistic understanding of the FBP by which it is developed and scaled up with a knowledge of the critical risks involved in manufacturing process analyzed by risk assessment tools like: Qualitative Initial Risk-based Matrix Analysis (IRMA) and Quantitative Failure Mode Effective Analysis (FMEA) to identify and rank parameters with potential to have an impact on In Process/Finished Product Critical Quality Attributes (IP/FP CQAs). These Critical Process Parameters (CPPs) were further refined by DoE and MVDA to develop design space with Real Time Release Testing (RTRT) that leads to implementation of a control strategy to achieve consistent finished product quality at lab scale itself to prevent possible product failure at larger manufacturing scale.
  7,665 784 2
Development of lyophilization cycle and effect of excipients on the stability of catalase during lyophilization
Shantanu V Lale, Monu Goyal, Arvind K Bansal
October-December 2011, 1(4):214-221
DOI:10.4103/2230-973X.93007  PMID:23071946
Introduction: The purpose of the present study was to screen excipients such as amino acids and non-aqueous solvents for their stabilizing effect on catalase, a model protein, for lyophilization. The present study also includes optimization of lyophilization cycle for catalase formulations, which is essential from the commercial point of view, since lyophilization is an extremely costly process. Materials and Methods: Activity of catalase was determined using catalase activity assay. Differential scanning calorimetry was used to determine eutectic melting temperature of the frozen catalase solution, which is essential for the optimization of lyophilization cycle. Results: When catalase was lyophilized without excipients, it was found that about 65-78% of the initial activity of catalase was lost during the lyophilization process in a concentration dependent manner. The maximum stability of catalase during lyophilization was observed at pH 7.0. Amino acids like alanine, glycine, lysine, serine and 4-hydroxy proline showed strong stabilizing effect on catalase during lyophilization by protecting catalase activity above 95%, whereas valine and cysteine hydrochloride showed destabilizing effect on catalase. Non-aqueous solvents such as dimethyl formamide, dimethyl sulphoxide, polyethylene glycol (PEG) 200, PEG 400, PEG 600 and ethylene glycol also showed destabilizing effect on catalase during lyophilization. Conclusions: In order to prevent loss of catalase activity during lyophilization of catalase, use of amino acids like alanine, glycine, lysine, serine and 4-hydroxy proline in optimum concentration is highly advisable.
  7,408 924 5
Design and development of a self-nanoemulsifying drug delivery system for telmisartan for oral drug delivery
Jaydeep Patel, Garala Kevin, Anjali Patel, Mihir Raval, Navin Sheth
April-June 2011, 1(2):112-118
DOI:10.4103/2230-973X.82431  PMID:23071930
Background and Aim: Telmisartan (TEL) is an angiotensin II receptor blocker (ARB) antihypertensive agent. The aim of the present investigation was to develop a self-nanoemulsifying drug delivery system (SNEDDS) to enhance the oral bioavailability of poorly water soluble TEL. Materials and Methods: The solubility of TEL in various oils was determined to identify the oil phase of a SNEDDS. Various surfactants and co-surfactants were screened for their ability to emulsify the selected oil. Pseudoternary phase diagrams were constructed to identify the efficient self-emulsifying region. A SNEDDS was further evaluated for its percentage transmittance, emulsification time, drug content, phase separation, dilution, droplet size, zeta potential, pH, refractive index, and viscosity. Results: The developed SNEDDS formulation contained TEL (20 mg), Tween; 20 (43.33%w/w), Carbitol; (21.67%w/w), and Acrysol; EL 135 (32%w/w). The optimized formulation of the TEL-loaded SNEDDS exhibited a complete in vitro drug release in 15 min as compared with the plain drug, which had a limited dissolution rate. It was also compared with the pure drug suspension by oral administration in male Wister rats. The in vivo study exhibited a 7.5-fold increase in the oral bioavailability of TEL from the SNEDDS compared with the pure drug suspension. Conclusions: These results suggest the potential use of the SNEDDS to improve the dissolution and oral bioavailability of poorly water soluble TEL.
  6,653 1,262 10
Cavamax W7 composite psoralen ethosomal gel versus cavamax W7 psoralen solid complex gel for topical delivery: A comparative evaluation
Smriti Kumari, Kamla Pathak
October-December 2013, 3(4):171-182
DOI:10.4103/2230-973X.121284  PMID:24350036
Aim: The present research work was aimed to formulate and characterize psoralen-encapsulated cavamax W7 composite ethosomal gel and compare its in vitro and ex vivo behavior against psoralen-cavamax W7-complex reference gel. Materials and Methods: A total of nine formulations of composite ethosomes were prepared by injection method using 3 2 factorial design and entrapment efficiency was designated as dependent variable. Concomitantly, psoralen was complexed with cavamax W7 (1:1 molar ratio) by kneading method and formation of complex was confirmed by Diffuse reflectance spectroscopy (DRS), scanning electron microscopy (SEM), X-ray diffraction (XRD), and differential scanning calorimetry (DSC). Results: F9 with vesicle size of 183 ± 2.8 nm, and highest % entrapment efficiency of 98.12 ± 1.15 was selected as optimized formulation. Transmission electron microscopy (TEM) revealed uniform and spherical shaped vesicles. The optimized formulation F9 was formulated as carbapol gel and compared against ethosomal gel, psoralen gel, and psoralen cavamax W7 complex gel. The gels were evaluated for permeation characteristics and the rank order was composite ethosomal gel > ethosomal gel > psoralen-cavamax W7 complex gel > psoralen gel. The ethosomal gel (G5) with highest in vitro permeation of 82.48 ± 2.23% was subjected to in vivo Confocal laser scanning microscopy (CLSM) studies using rhodamine B as tracer. The penetration of rhodamine B was uniform, deeper, and two times faster into epidermis than control gel. Conclusion: Conclusively, cavamax W7 composite ethosomes present themselves as efficient carrier for superior topical delivery of psoralen and have potential for clinical applications in minimizing side effects associated with photosensitivity of psoralen.
  2,258 5,588 1
Formulation and evaluation of microemulsion-based hydrogel for topical delivery
Vidya Sabale, Sejal Vora
July-September 2012, 2(3):140-149
DOI:10.4103/2230-973X.104397  PMID:23373005
Background: The purpose of this study was to develop microemulsion-based hydrogel formulation for topical delivery of bifonazole with an objective to increase the solubility and skin permeability of the drug. Materials and Methods: Oleic acid was screened as the oil phase of microemulsions, due to a good solubilizing capacity of the microemulison systems. The pseudo-ternary phase diagrams for microemulsion regions were constructed using oleic acid as the oil, Tween 80 as the surfactant and isopropyl alcohol (IPA) as the cosurfactant. Various microemulsion formulations were prepared and optimized by 3 2 factorial design on the basis of percentage (%) transmittance, globule size, zeta potential, drug release, and skin permeability. The abilities of various microemulsions to deliver bifonazole through the skin were evaluated ex vivo using Franz diffusion cells fitted with rat skins. The Hydroxy Propyl Methyl Cellulose (HPMC) K100 M as a gel matrix was used to construct the microemulsion-based hydrogel for improving the viscosity of microemulsion for topical administration. The optimized microemulsion-based hydrogel was evaluated for viscosity, spreadability, skin irritancy, skin permeability, stability, and antifungal activity by comparing it with marketed bifonazole cream. Results: The mechanism of drug release from microemulsion-based hydrogel was observed to follow zero order kinetics. The studied optimized microemulsion-based hydrogel showed a good stability over the period of 3 months. Average globule size of optimized microemulsion (F5) was found to be 18.98 nm, zeta potential was found to be -5.56 mv, and permeability of drug from microemulsion within 8 h was observed 84%. The antifungal activity of microemulsion-based hydrogel was found to be comparable with marketed cream. Conclusion: The results indicate that the studied microemulsion-based hydrogel (F5) has a potential for sustained action of drug release and it may act as promising vehicle for topical delivery of ibuprofen.
  6,387 1,409 15
Dissolution enhancement of efavirenz by solid dispersion and PEGylation techniques
B Bindu Madhavi, B Kusum, CH Krishna Chatanya, M Naga Madhu, V Sri Harsha, David Banji
January-March 2011, 1(1):29-34
DOI:10.4103/2230-973X.76726  PMID:23071917
Background: Efavirenz is the preferred nonnucleotide reverse transcriptase inhibitor for first-line antiretroviral treatment in many countries. It is orally active and is specific for human immunodeficiency virus type 1. Its effectiveness can be attributed to its long half-life, which is 52-76 h after multiple doses. The drug is having poor water solubility. The formulation of poorly soluble drug for oral delivery will be one of the biggest challenges for formulation scientists in the research field. Among the available approaches, the solid dispersion technique has often proved to be the most commonly used method in improving dissolution and bioavailability of the drugs because of its simplicity and economy in preparation and evaluation. Materials and Methods: Solid dispersions were prepared by solvent evaporation and physical mixture methods by using polyethylene glycol as the hydrophilic carrier and PEGylated product was also prepared. The prepared products were evaluated for various parameters, such as polymer interaction, saturation solubility study, and drug release studies. The drug release data were analyzed by fitting it into various kinetic models. Results: There is an improvement in the dissolution from 16% to 70% with solid dispersion technology. Higuchi model was found to be the best fit model. Conclusion: Solid dispersion is the simple, efficient, and economic method to improve the dissolution of the poorly water-soluble drugs.
  6,273 1,379 12
Mucoadhesive buccal films of glibenclamide: Development and evaluation
Y Indira Muzib, K Srujana Kumari
January-March 2011, 1(1):42-47
DOI:10.4103/2230-973X.76728  PMID:23071919
Background : Glibenclamide is an oral hypoglycemic drug completely metabolized in the liver, the principal metabolite being very weakly active, buccal delivery may be useful for the treatment of diabetes more effectively. The aim of the present study was to design formulations and systematically evaluate in vitro and ex vivo performances of buccal films of glibenclamide so that the required therapeutic plasma concentrations can possibly be achieved more rapidly using the different grades of hydroxypropyl methyl cellulose (HPMC) as the base matrix. Materials and Methods: Mucoadhesive buccal films of glibenclamide were prepared by solvent casting technique using different grades of HPMC with different ratios. Prepared films were evaluated for weight, thickness, surface pH, swelling index (SI), folding endurance, drug content uniformity, in vitro release, and ex vivo permeation studies. Results: The film thickness and weight were in the range of 0.213-0.4892mm and 22.25-39.83 mg, respectively. The films exhibited controlled release over more than 6 h. HPMC, HPMCK100, and HPMC3000 films exhibited satisfactory swelling. Surface pH of buccal films was found to be 6.4-6.8. SI observed to be highest for GF12 (275.3 ± 12.17) and lowest for GF1 (173.5 ± 5.65). The films exhibited controlled release over more than 6 h. HPMC exhibited satisfactory swelling, an optimum residence time, and promising drug release. The Higuchi plots were found to be linear with correlation coefficient values of 0.8933, 0.9138, and 0.9947 for GF4, GF8, and GF9, respectively. Conclusions: Among all the formulations, GF9 shows good controlled release results correlated with ex vivo permeation studies.
  6,455 1,175 10
A perspective overview on lipospheres as lipid carrier systems
Thushara Bindu Dudala, Prasanna Raju Yalavarthi, Harini Chowdary Vadlamudi, Jyotsna Thanniru, Gowri Yaga, Naga Lakshmi Mudumala, Vivek Kumar Pasupati
October-December 2014, 4(4):149-155
Both hydrophilic and lipophilic therapeutics can be delivered successfully into deep and peripheral tissues such as cerebrospinal fluid and central nervous system by encapsulating them with crystalline lipids as lipospheres. The advent of lipospheres was meant to deliver both therapeutic moieties with enhanced efficacy and added stability to reach out intended tissue areas. Although extensive information is available on physicochemical, analytical and biopharmaceutical aspects of lipospheres, there was no specific order pertaining to critical composition and rationale of component selection available for academic and pilot scale processing of lipospheres. With the interest of compiling key points in a typical formulation of lipid lipospheres, this article was intrigued to discuss melt method, co-solvent, microemulsion, super critical fluid, spray drying and spray congealing techniques that were employed to scale up lipospheres. The selection criteria for both the drugs and lipids in liposphere formulations were demonstrated here. The quality assessment with variables like loading capacity and entrapment efficiency was explained. A note on preliminary screening factors to determine the liposphere formation such as liposphere dimensions with morphological scenario was detailed in this article. This article also includes the stability and storage issues with reference to photolysis. The marked differential in enhancing solubility and permeability characteristics of Class II and IV drug candidates by liposphere delivery systems with an evident of in vivo outcomes were emphasized.
  2,066 5,519 5
Improvement in solubility of poor water-soluble drugs by solid dispersion
Swati Sareen, George Mathew, Lincy Joseph
January-March 2012, 2(1):12-17
DOI:10.4103/2230-973X.96921  PMID:23071955
This article is intended to combine recent literature on solid dispersion technology for solubility enhancement with special emphasis on mechanism responsible for the same by solid dispersion, various preparation methods, and evaluation parameters. Solubility behavior is the most challenging aspect for various new chemical entities as 60% of the new potential products possess solubility problems. This is the biggest reason for new drug molecules not reaching to the market or not reaches to full potential. There are various techniques to enhance the drug solubility such as particle size reduction, nanosuspension, use of surfactants, salt formation, solid dispersion, etc. From this article it may be concluded that solid dispersion is an important approach for improvement of bioavailability of poor water-soluble drugs.
  6,490 1,019 22
Developing micro-/nanoparticulate drug delivery systems using "design of experiments"
Bhupinder Singh, Rahul Bhatowa, Chandra Bhushan Tripathi, Rishi Kapil
April-June 2011, 1(2):75-87
DOI:10.4103/2230-973X.82395  PMID:23071925
Of late, micro and nanoparticluate drug delivery systems have been gaining immense importance primarily attributed to their improved drug release controlling and targeting efficiencies. Also, the small particle size and desirable surface charge associated with these delivery systems render them suitable for specific applications like lymphatic uptake, pulmonary uptake, tumor targeting, brain targeting, etc. For decades, micro and nanoparticulate systems have been prepared by the conventional "trial and error" approach of changing One Variable at a Time (OVAT). Using this methodology, the solution of a specific problematic formulation characteristic can certainly be achieved, but attainment of the true optimal composition is never guaranteed. Thus, the present manuscript provides an updated account of the systematic approach "Design of Experiments (DoE)" as applicable to formulation development of microparticles and nanostructured systems. Besides providing a bird's eye view of the various experimental designs and optimization techniques employed for DoE optimization of such systems, the present manuscript also presents a copilation of the major micro/nano-structuctred systems optimized through DoE till date. In a nutshell, the article will act both as a ready reckoner of DoE optimization of micro/nano drug delivery systems and a catalyst in providing an impetus to young pharmaceutical "nano & micro" researchers to venture into the rewarding field of systematic DoE optimization.
  6,159 1,237 10
Formulation and evaluation of periodontal in situ gel
Kevin Garala, Parth Joshi, Malay Shah, A Ramkishan, Jaydeep Patel
January-March 2013, 3(1):29-41
DOI:10.4103/2230-973X.108961  PMID:23799203
Background: The present study was aimed to develop and optimize in situ gel for the treatment of periodontal disease. Materials and Methods: Temperature-sensitive in situ gel containing 0.1% w/v Chlorhexidine hydrochloride was formulated by cold method using different polymers. Preliminary study was carried out to optimize different types and concentration of polymers such as Poloxamer 188, Poloxamer 407, Gellan gum, and Carbopol 934P. Central composite design was employed for optimization of the effect of independent variables such as Poloxamer 407 and Carbopol 934P on responses such as gelation temperature, spreadability, cumulative percentage release at 2 h, and time for 50% drug release (t 50 %). Each formulations were evaluated for clarity, pH, gelation temperature, spreadability, drug content, in vitro drug release, t 50 %, and cumulative percentage drug release at 2 h. Results: Results of evaluation parameters revealed that the drug release, gelation temperature was considerably decreased with increasing t 50 % as the concentration of each polymer was increased. The desirability function was utilized to find out optimized formulation of the factorial design. Formulation F6 showed the highest overall desirability of 0.6283 and, therefore, this formulation was considered to be the optimized formulation. The % relative error was calculated, which showed that observed responses were in close agreement with the predicted values calculated from the generated regression equations. Conclusion: The clarity, pH, drug content of all formulations was found to be satisfactory. Further, all the formulations showed sustained drug release for a period of 6 h, which satisfied to treat periodontal disease.
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Nanocarrier-based hydrogel of betamethasone dipropionate and salicylic acid for treatment of psoriasis
Sanjula Baboota, Md Sarfaraz Alam, Shrestha Sharma, Jasjeet K Sahni, Anil Kumar, Javed Ali
July-September 2011, 1(3):139-147
DOI:10.4103/2230-973X.85963  PMID:23071936
Introduction: Betamethasone dipropionate (BD) has anti-inflammatory, immunomodulatory, and antiproliferative activity. The aim of the current work was to test the hypothesis that the addition of corticosteroid such as BD and a keratolytic agent such as salicylic acid in nanocarrier based microemulsions formulation would result in enhancement and sustaining of corticosteroid delivery rate leading to better anti-psoriatic activity. Clinical use of BD is restricted to some extent due to its poor permeability across the skin. So to increase its permeation across the skin, microemulsion-based gel formulations were prepared and characterised. Materials and Methods: Microemulsions were prepared by aqueous phase titration method, using oleic acid:sefsol (1.5:1), Tween 20, isopropyl alcohol, and distilled water as the oil phase, surfactant, cosurfactant and aqueous phase, respectively. Selected formulations were subjected to physical stability studies and consequently in vitro skin permeation studies. Surface studies of optimized formulation were done by transmission electron microscopy. In vivo anti-inflammatory activity was done by carageenan-induced raw paw edema method. Results: The droplet size of microemulsions ranged from 60 to 190 nm. The optimized formulation exhibited viscosity 28.55 ± 2.03 mP, refractive index 1.409, pH 6.4, and conductivity 10 -4 scm -1 . The optimized microemulsion was converted into hydrogel using carbopol 934, and salicylic acid was incorporated into it. Drug deposition in skin was found to be 29.73 μg/mg. Assessment of skin permeation was done by histopathology studies which indicated changes in the structure of epidermal membrane of skin. In vivo anti-inflammatory activity indicated 72.11% and 43.96% inhibition of inflammation in case of developed microemulsion gel and marketed gel, respectively. Conclusions: The developed microemulsion gel containing BD and salicylic acid provided sustained and good anti-inflammatory activity for the treatment of psoriasis.
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Formulation and evaluation of an in situ gel-forming ophthalmic formulation of moxifloxacin hydrochloride
Sonjoy Mandal, Manjunath KMJ Thimmasetty, GL Prabhushankar, MS Geetha
April-June 2012, 2(2):78-82
DOI:10.4103/2230-973X.100042  PMID:23119236
Background/Aim: The aim of the present investigation is to prepare and evaluate in situ gel-forming ophthalmic drug delivery system of moxifloxacin hydrochloride. Materials and Methods: Sodium alginate, a novel ophthalmic gel-forming mucoadhesive polymer, which gets converted to gel in the presence of divalent-cations (calcium ion) present in the lachrymal fluid, was used as the gelling agent. Hydroxy propyl methyl cellulose (HPMC) is a mucoadhesive polymer used as viscosity enhancer. Suitable concentrations of buffering agents were used to adjust the pH to 6.5. All the formulations were sterilized in an autoclave at 121°C for 15 minutes. The formulations were evaluated for clarity, pH measurement, gelling capacity, drug content estimation, rheological study, in vitro diffusion study, antibacterial activity, isotonicity, and eye irritation study. Results: The developed formulations exhibited sustained release of drug from formulation over a period of 10 hours thus increasing residence time of the drug. The optimized formulations were tested for eye irritation on albino rabbit (male). The formulations were found to be non-irritating with no ocular damage or abnormal clinical signs to the cornea, iris or conjunctiva observed. Conclusion: These in situ gelling systems containing gums may be a valuable alternative to the conventional systems.
  5,781 1,090 17
A comprehensive study on regulatory requirements for development and filing of generic drugs globally
Shweta Handoo, Vandana Arora, Deepak Khera, Prafulla Kumar Nandi, Susanta Kumar Sahu
July-September 2012, 2(3):99-105
DOI:10.4103/2230-973X.104392  PMID:23373001
The regulatory requirements of various countries of the world vary from each other. Therefore, it is challenging for the companies to develop a single drug which can be simultaneously submitted in all the countries for approval. The regulatory strategy for product development is essentially to be established before commencement of developmental work in order to avoid major surprises after submission of the application. The role of the regulatory authorities is to ensure the quality, safety, and efficacy of all medicines in circulation in their country. It not only includes the process of regulating and monitoring the drugs but also the process of manufacturing, distribution, and promotion of it. One of the primary challenges for regulatory authority is to ensure that the pharmaceutical products are developed as per the regulatory requirement of that country. This process involves the assessment of critical parameters during product development.
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