Due to lack of specification and solubility of drug molecules, patients have to take high doses of the drug to achieve the desired therapeutic effects for the treatment of diseases. To solve these problems, there are various drug carriers present in the pharmaceuticals, which can used to deliver therapeutic agents to the target site in the body. Mesoporous silica materials become known as a promising candidate that can overcome above problems and produce effects in a controllable and sustainable manner. In particular, mesoporous silica nanoparticles (MSNs) are widely used as a delivery reagent because silica possesses favorable chemical properties, thermal stability, and biocompatibility. The unique mesoporous structure of silica facilitates effective loading of drugs and their subsequent controlled release of the target site. The properties of mesoporous, including pore size, high drug loading, and porosity as well as the surface properties, can be altered depending on additives used to prepare MSNs. Active surface enables functionalization to changed surface properties and link therapeutic molecules. They are used as widely in the field of diagnosis, target drug delivery, bio-sensing, cellular uptake, etc., in the bio-medical field. This review aims to present the state of knowledge of silica containing mesoporous nanoparticles and specific application in various biomedical fields.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Introduction: The copolymer of polyethylene glycol (PEG) and polyesters has many interesting properties, such as amphiphilicity, biocompatibility, biodegradability, and self-assembly in an aqueous environment. Diblock copolymers of PEG-polyester can form different structures such as micelles, polymersome, capsules or micro-container in an aqueous environment according to the length of their blocks. Materials and Methods: Herein, a series of poly (lactic acid) (PLA) and PEG diblock copolymers were synthesized through the ring-opening polymerization. The polymerization reaction and the copolymer structures were evaluated by nuclear magnetic resonance (NMR) and gel permeation chromatography (GPC). The corresponding copolymers were implemented for the formation of polymersome structures using film rehydration method. Impact of methoxy PEG chain length and hydrophobic weight fraction on particle size of polymersomes were studied, and the proper ones were selected for loading of doxorubicin (DOX) via pH gradient method. Results and Discussion: Results obtained from ¹ HNMR and GPC revealed that microwave irradiation is a simple and reliable method for the synthesis of PEG-PLA copolymers. Further analysis indicated the copolymer with relative molecular weight of PLA to PEG ratios of 3 or f_Eo ~ 25% produced the smallest size polymersomes. Polymersomes prepared from PEG ₅₀₀₀ to PLA ₁₅₀₀₀ were more capable in loading and sustained release of DOX than those prepared from PEG ₂₀₀₀ to PLA ₆₀₀₀ . Conclusion: In conclusion copolymers of PEG/PLA with f_OE ~25% and relatively higher molecular weight are more suitable for encapsulation and providing sustained release of DOX.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Nanotechnology is directed at manipulating matter at the nanometer level and the application of the same to medicine is called nanomedicine. Over the past few years researchers have developed various nanomedicines for diagnosis, prevention as well as cure of various ailments both locally and systemically. In dentistry, drug loaded nanopharmaceuticals based on nanomaterials have been utilized extensively over the past few years to cure dental problems and facilitate attainment of a near-perfect oral hygiene. Although various drug delivery systems have already been investigated for treating periodontitis, research is currently focused on nanodelivery systems for efficient targeted delivery of drugs to the periodontal pocket. In this context a few nanodelivery systems explored include nanocomposite hydrogels, nanoparticles, nanoemulsion etc. A number of herbal and synthetic drugs examples of which include trichlosan, tetracycline, Harungana madagascariensis leaf extract, minocycline, metronidazole, chlorhexidine have been encapsulated into nanodelivery systems for treating periodontitis. A few examples of polymers investigated as matrices for the delivery of drugs to the periodontal pocket include chitosan, Poly lactic-co-glycolic acid copolymer, poly e caprolactone, polylactic acid, polypropylene, cellulose acetate propionate and ethyl vinyl acetate. In the near future also nanotechnology is expected to find its application in all the specializations of dentistry ranging from diagnosis and treatment of oral cancers to development of colloidal suspension containing millions of active analgesic micron-size dental robots resulting in anesthesia in patients. In the light of the above facts the current editorial focuses on the applications of nanotechnology based nanomedicines which cannot be undermined in the improvement of dental health and hygiene both, in the current as well as in future scenario.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Introduction: Ketorolac tromethamine (KT), a nonsteroidal anti-inflammatory drug, when given orally causes gastrointestinal disturbances. Its transdermal drug delivery may reduce such side effects associated with them. The present investigation was aimed at evaluating the efficiency of various penetration enhancers for improved permeation of KT through the skin. Materials and Methods: A concentration of 1 mg/mL of the drug solution with enhancers was used to evaluate diffusion through the rat skin using a Franz diffusion cell assembly. 20 different penetration enhancers were selected for this study. Results: Saturated fatty acids like stearic and palmitic acid were found to increase the permeation rate of the drug to a great extent whereas unsaturated fatty acid viz. oleic acid exhibited maximum permeation. Increase in permeability efficiency of various penetration enhancers was observed in the following order: Oleic acid > stearic acid > palmitic acid > isopropyl myristate > tween 80 > span 80 > span 40 > span 20 > l-limonene > l-menthol > fenchone > α-pinene > urea > dimethyl sulfoxide (DMSO) > triton X-100 > tween 20 > dimethyl formamide > acetone > control > citric acid > ascorbic acid. Ascorbic acid and citric acid had no effect on permeation rate. Conclusion: The results revealed that the permeation of KT through the skin can maximally be enhanced using oleic acid-an unsaturated fatty acid.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

The objective of the present work was to develop a novel delivery system of ketorolac tromethamine (KT) for dual pulse release based on microspheres and tablet in capsule system (MATICS) as a treatment modality for rheumatoid arthritis. The design consisted of an impermeable hard gelatin capsule body, in which a core tablet was (second pulse) placed in the bottom and sealed with a hydrogel plug (HP2). The body was locked with enteric coated cap filled with KT microspheres (first pulse). The microspheres for first pulse were selected by screening the formulations (M1-M6), and M1 with least particle size of 96.38 ± 0.05 μm, highest drug loading of 25.10% ± 0.28% and maximum CDR of 89.32% ± 0.21% was adjudged as the best formulation. The HP2 tablet was selected based on its capability for maintaining a lag period of 6 h. The selection criterion of the second pulse (core tablet: T3) was its disintegration time of 4.02 ± 0.53 min and CDR of 99.10% ± 0.32% in 30 min. All the optimized formulations were assembled in accordance with the proposed design to form pulsatile MATICS and evaluated for in vitro release. MATICS displayed delayed sustained CDR of 80.15% in 8 h from the first pulse (microspheres) after a lag time of 2 h, followed by 97.05% KT release from second pulse (core tablet) in simulated colonic fluid within 10 h. Conclusively, in vitro pulsatile release was a rational combination of delayed sustained and immediate release of KT that has the potential to combat the pain at night and morning stiffness. Incorporation of two pulses in one system offers a reduction in dose frequency and better pain management.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Aim: The objective of the current study is to increase the dissolution rate of cefuroxime axetil (CA) by formation of binary CA solid dispersion using water soluble carriers such as polyvinylpyrrolidone (PVP K30) and polyethylene glycol (PEG 4000). Methods: Solid dispersions (SDs) between CA and PVP K30/PEG 4000 were formed by dissolving both compounds in a common solvent, methanol, which were rotary evaporated at 40°C for 12 h. Physical mixtures between CA and PVP K30/PEG 4000 were also formulated as to compare the efficiency of SDs. The physicochemical properties of CA and all its formulations were then characterized using differential scanning calorimetric analysis (DSC), powder X-ray diffraction studies (PXRD), and Fourier transform infrared spectroscopy (FTIR). Results: All SD formulations were found to have a higher dissolution rate comparatively to pure CA, while only physical mixtures of PVP K30 were found having a significantly higher dissolution rate. The enhancement of dissolution rate SD by PVP K30 may be caused by increase wettability, solubility, reduction in particle size or the formation of CA β crystalline. Increment of dissolution rate of CA SDs by PEG 4000 similarly may be caused by increase wettability, solubility, and reduction in particle size. This phenomenon may also be caused by amorphization as suggested by DSC and PXRD. Conclusions: The SD of CA with PVP K30 and PEG 4000, lends an ample credence for better therapeutic efficacy.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Aim and Objectives: In the present investigation dual agents i.e., hesperidin and diazepam loaded polymeric nanoparticles (NPs) were formulated by nanoprecipitation method and optimized using three-level factorial design. Methods: The developed NPs were optimized keeping poly (lactic-co-glycolic) acid (PLGA), poloxamer amount as independent process variable and z-average, percentage drug entrapment as a dependent response. The optimized NP was subjected to in vitro drug release study to investigate drug release mechanism from NP. Cell viability assay was performed on Vero cell line to confirm the safety of NP. Results: Drug loaded NP showed z-average in the range of 189-307 d.nm with percentage drug entrapment for diazepam and hesperidin 62-89% and 68-92%, respectively. In vitro drug release studies showed controlled drug release behavior was observed from polymeric NP across dialysis membrane compared to aqueous drug solution. Cell viability assay showed drug dependent cytotoxicity on Vero cell line, however, polymeric NP showed less cytotoxicity compared with aqueous drug solution.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]

Introduction: The objective of this investigation was to design and optimize the experimental conditions for the fabrication of camptothecin (CPT) loaded Eudragit S 100. Nanoparticles, and to understand the effect of various process parameters on the average particles size, particle size uniformity and surface area of the prepared polymeric nanoparticles using Taguchi design. Materials and Methods: CPT loaded Eudragit S 100 nanoparticles were prepared by nanoprecipitation method and characterized by particles size analyzer. Taguchi orthogonal array design was implemented to study the influence of seven independent variables on three dependent variables. Eight experimental trials involving seven independent variables at higher and lower levels were generated by design expert. Results: Factorial design result has shown that (a) except, β-cyclodextrin concentration all other parameters do not significantly influenced the average particle size (R1); (b) except, sonication duration and aqueous phase volume, all other process parameters significantly influence the particle size uniformity; (c) all the process parameters does not significantly influence the surface area. Conclusion: The R1, particle size uniformity and surface area of the prepared drug-loaded polymeric nanoparticles were found to be 120 nm, 0.237 and 55.7 m ² /g and the results were good correlated with the data generated by the Taguchi design method.

[ABSTRACT]  [FULL TEXT]  [PDF]  [Mobile Full text]  [EPub] [CITATIONS]  [PubMed]