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   Table of Contents - Current issue
October-December 2017
Volume 7 | Issue 4
Page Nos. 155-198

Online since Friday, April 6, 2018

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Lipid nanocapsules formulation and cellular activities evaluation of a promising anticancer agent: EAPB0503 Highly accessed article p. 155
Adrien Chouchou, Anne Aubert-Pouëssel, Christophe Dorandeu, Zahraa Zghaib, Pierre Cuq, Jean-Marie Devoisselle, Pierre-Antoine Bonnet, Sylvie Bégu, Carine Deleuze-Masquefa
Objective: EAPB0503, lead compound of imiqualines, presented high antitumor activities but also a very low water solubility which was critical for further preclinical studies. To apply to EAPB0503, a robust and safe lipid formulation already used for poor soluble anticancer agents for injectable administration at a concentration higher than 1 mg/mL. Materials and Methods: Physicochemical properties of EAPB0503 were determined to consider an adapted formulation. In a second time, lipid nanocapsules (LNC) formulations based on the phase-inversion process were developed for EAPB0503 encapsulation. Then, EAPB0503 loaded-LNC were tested in vitro on different cell lines and compared to standard EAPB0503 solutions. Results: Optimized EAPB0503 LNC displayed an average size of 111.7 ± 0.9 nm and a low polydispersity index of 0.059 ± 0.002. The obtained loading efficiency was higher than 96% with a drug loading of 1.7 mg/mL. A stability study showed stability during 4 weeks stored at 25°C. In vitro results highlighted similar efficiencies between LNC and standard EAPB0503 solutions prepared in dimethyl sulfoxide. Conclusion: In view of results obtained for loading efficiency and drug loading, the use of a LNC formulation is very interesting to permit the solubilization of a lipophilic drug and to improve its bioavailability. Preliminary tested pharmaceutical formulation applied to EAPB0503 significantly improved its water solubility and will be soon considered for future preclinical in vivo studies.
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Formulation of cilostazol spherical agglomerates by crystallo-co-agglomeration technique and optimization using design of experimentation p. 164
Sanjeevani Shekhar Deshkar, Govind R Borde, Rupali N Kale, Balasaheb A Waghmare, Asha Biju Thomas
Introduction: Spherical agglomeration is one of the novel techniques for improvement of flow and dissolution properties of drugs. Cilostazol is a biopharmaceutics classification system Class II drug with poor solubility resulting in limited bioavailability. The present study aims at improving the solubility and dissolution of cilostazol by crystallo-co-agglomeration technique. Materials and Methods: Cilostazol agglomerates were prepared using various polymers with varying concentration of hydroxypropyl methylcellulose E 50 (HPMC E50), polyvinyl pyrrolidone K30 (PVP K30), and polyethylene glycol 6000. The influence of polymer concentration on spherical agglomerate formation was studied by 32 factorial design. Cilostazol agglomerates were evaluated for percent yield, mean particle size, drug content, aqueous solubility, and in vitro dissolution and further characterized by Fourier transform infrared spectroscopy (FTIR), scanning electron microscopy (SEM), differential scanning calorimetry (DSC), and X-ray diffraction (XRD). Results: The agglomeration process resulted in optimized formulation, F3 with mean agglomerate size of 210.0 ± 0.56 μm, excellent flow properties, approximately 15-fold increase in solubility than pure cilostazol and complete drug release in 60 min. Process yield, agglomerate size, and drug release were affected by amount of PVP K 30 and HPMC E50. The presence of drug microcrystal was confirmed by SEM, whereas FTIR study indicated no chemical change. Increase in drug solubility was attributed to change of crystalline drug to amorphous form that is evident in DSC and XRD. Conclusion: Crystallo-co-agglomeration can be adopted as an important approach for increasing the solubility and dissolution of poorly soluble drug.
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Aminopropyl groups of the functionalized Mobil Crystalline Material 41 as a carrier for controlled diclofenac sodium and piroxicam delivery p. 174
Elham Khodaverdi, Mina Ahmadi, Hossein Kamali, Farzin Hadizadeh
Objective: Synthetic Mobil Crystalline Material 41 (MCM-41) as a mesoporous material and functionalized MCM-41 using aminopropyl groups were studied in order to investigate their ability to encapsulate and to control the release of diclofenac sodium and piroxicam. Materials and Methods: MCM-41 was synthesized through sol–gel procedure and functionalized with aminopropyl groups. The physicochemical properties of MCM-41 were studied through particle size analysis, infrared spectroscopy, scanning electron microscopy, transmission electron microscopy, and carbon–hydrogen–nitrogen analysis. Diclofenac sodium and piroxicam were loaded into the MCM-41 matrix using the filtration and solvent evaporation methods. The drug-loading capacity was determined by ultraviolet, Fourier transform infrared, X-ray diffraction, and Brunauer–Emmett–Teller analysis. Results: According to the results for pure drug release, >57% was released in the 1st h, but when these drugs were loaded into pure Mobil Crystalline Material 41 (MCM-41) and functionalized MCM-41, the release into the simulated gastrointestinal medium was less, continuous, and slower. The release of piroxicam from functionalized MCM-41 was slower than that from MCM-41 in the simulated intestinal medium because of the formation of electrostatic bonds between piroxicam and the aminopropyl groups of the functionalized MCM-41. However, in the case of diclofenac sodium, there was no significant difference between pure MCM-41 and functionalized MCM-41. The difference between piroxicam and diclofenac sodium was due to the high solubility of diclofenac sodium in the intestinal medium (pH 6.8), which caused more rapid release from the matrixes than for piroxicam. Conclusion: Our findings indicate that, after functionalization of MCM-41, it could offer a good means of delivering controlled diclofenac sodium and piroxicam.
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Drug information center as referral service in a South Indian tertiary care hospital p. 182
Sapan Kumar Behera, Alphienes Stanley Xavier, Vikneswaran Gunaseelan, Byrappa Kempalalakshmamma Ravindra, Sandhiya Selvarajan, Adithan Chandrasekaran, Steven Aibor Dkhar
Objective: The objective of this study is to assess the various aspects of drug information services (DISs) provided in the DI center of a tertiary care hospital. Materials and Methods: DI queries received from various departments from April 2013 to May 2017 were included in the study. Various aspects such as year- and department-wise distribution, reason for sending the queries, mode of receipt and reply, time taken for reply, number of visit for bedside examination of patients, and number of references given per query were analyzed. All the results are expressed in numbers and percentages. Results: Fifty-five DI queries were received during the study period. Most of the queries were received from Department of Orthopedics (26, 47.27%), followed by Neurology (4, 7.27%). Most common mode of receipt of queries (41, 74.55%) was by Cross-reference form not case record form followed by phone calls (8, 14.55%) and outpatient department (OPD) case sheet (6, 10.9%). CRF with attached opinion was the most common mode of reply (41, 74.55%) followed by phone calls (7, 12.73%), and OPD case sheets (6, 10.9%). The most common reason for sending queries was antimicrobials-related problem (25, 45.46%), followed by the use of anticoagulants (13, 23.63%). Most of the queries were replied within 24 h (31, 56.36%), followed by 48 h (14, 25.45%). Out of 41 CRF received for in-patients, bedside examination was requested in 23 (56.09%) CRF. There was an increasing trend in the number of queries received every year with more queries received during 2016 (23, 41.82%). Conclusions: DIS if utilized properly can be used as a referral service such as other specialties in a tertiary care hospital.
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Effect of local application of curcumin and ornidazole gel in chronic periodontitis patients p. 188
PL Ravishankar, Y Pradeep Kumar, EN Anila, Priyankar Chakraborty, Maharshi Malakar, R Mahalakshmi
Objective: The objective of this study is to evaluate the comparative effect of curcumin and ornidazole in treating chronic periodontitis. Materials and Methods: Twenty individuals of both sexes aged between 27 and 53 years diagnosed with chronic periodontitis and having pocket depths >5 mm bilaterally were selected for this study, in a split-mouth design. Examination of plaque index, probing pocket depth, and clinical attachment level was measured for each patient. The patients received a complete prophylaxis including scaling and root planing after which, both test gels were injected into the two experimental sites chosen, that had probing depth (PD) >5 mm and were located in symmetric quadrants. Pocket PD, clinical attachment loss, and plaque index were recorded at days 0 and 30. Results: At 1-month evaluation, curcumin group showed a significant decrease in pocket PD, plaque index, and clinical attachment loss when compared to the ornidazole group. Conclusion: The results show a more favorable outcome with curcumin than ornidazole gel, thus curcumin can be used as an adjunct to nonsurgical periodontal therapy.
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An assessment of reported adverse drug reactions in a Tertiary Care Hospital in South India: A retrospective cross-sectional study p. 193
Sandeep Kumar Gupta, K Deva Kumar
Objective: The primary objective of this study was to assess the causality of ADRs using World Health Organization-Uppsala Monitoring Centre (WHO–UMC), Naranjo and Liverpool ADR Causality Assessment Tool (LCAT). Other primary objective was to assess the agreement between the WHO-UMC criterion, Naranjo algorithm and LCAT. The secondary objective was to assess the reported adverse drug reactions in a tertiary care hospital in South India. Materials and Methods: This was a cross-sectional retrospective study. All the ADRs which were reported by the Pharmacovigilance Unit between July 2016 and March 2017 were assessed. Causality assessment was performed by two well-trained independent pharmacologists by applying the three methods–WHO, Naranjo and LCAT. Concurrence between the two algorithms was compared using the Cohen's weighted kappa statistic. Results: Causality assessment of adverse reactions according to Naranjo criteria shows that 81% cases were of probable type, 9.5% cases were possible and 9.5% cases were unlikely. Causality assessment of adverse reactions according to WHO-UMC criteria shows that 85.7% cases were of probable type, 4.8% cases were possible, 4.8% cases were unlikely and 4.8% cases were definite. Causality assessment of adverse reactions according to Liverpool criteria shows that 61.9% cases were of probable type, 4.8% cases were possible and 33.3% cases were definite. Cohen's kappa test shows that negative and poor concurrence was seen between WHO and Naranjo causality comparison (κ = −0.161). Positive but poor concurrence based on kappa values was seen between Liverpool and Naranjo's causality comparison (κ = 0.133). Negative and poor concurrence based on kappa values was seen between WHO and Liverpool causality comparison (κ = −0.161). Conclusion: The most frequent causality category observed by the WHO-UMC criteria, Naranjo as well as the Liverpool algorithm was “Probable.” Full concurrence was not found between any of two scales of causality assessment.
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Erratum: Development of a binary carrier system consisting polyethylene glycol 4000 - ethyl cellulose for ibuprofen solid dispersion p. 198

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