Albumin nanoparticles coated with polysorbate 80 as a novel drug carrier for the delivery of antiretroviral drug-Efavirenz.

PURPOSE OF THE STUDY: The antiretroviral therapy (ART) has dramatically improved human immunodeficiency virus (HIV)/acquired immunodeficiency syndrome (AIDS) treatment, prevention and also has been found to increase the lifespan of HIV/AIDS patients by providing durable control of the HIV replication in patients. Efavirenz is a non-nucleoside reverse transcriptase inhibitor of HIV-1. The purpose of this study is to formulate efavirenz-loaded bovine serum albumin nanoparticles to improve efavirenz delivery into various organs. MATERIALS AND METHODS: Nanoparticles were prepared by desolvation technique and coated with polysorbate 80. Ethanol, glutaraldehyde, and mannitol were used as desolvating, cross linking agent, and cryoprotectant, respectively. Drug to polymer ratio was chosen at five levels from 1:2, 1:3, 1:4, 1:5, and 1:6 (by weight). The formulated nanoparticles were characterized for Fourier Transform Infrared (FT-IR) spectroscopy, differential scanning calorimetry (DSC) studies, entrapment efficiency, particle size, surface charge, surface morphology, in vitro drug release, release kinetics, stability studies, and biodistribution studies. RESULTS AND MAJOR CONCLUSION: The particle size of the prepared formulations was found below 250nm with narrow size distribution, spherical in shape and showed good entrapment efficiency (45.62-72.49%). The in vitro drug release indicated biphasic release and its data were fitted to release kinetics models and release pattern was Fickian diffusion controlled release profile. The prepared nanoparticles increased efavirenz delivery into various organs by several fold in comparison with the free drug.

Albumin nanoparticles for the delivery of gabapentin: preparation, characterization and pharmacodynamic studies.

The study was aimed to prepare and evaluate gabapentin loaded albumin nanoparticles and to find out their effectiveness in treating epilepsy. Albumin nanoparticles of gabapentin were prepared by pH-coacervation method. The drug was administered into animals as free drug, gabapentin bound with nanoparticles, and gabapentin bound with nanoparticles coated with polysorbate 80. The polysorbate 80 coated nanoparticles increased the gabapentin concentration in the brain about 3 fold in comparison with the free drug. Moreover, the polysorbate 80 coated nanoparticles significantly reduced the duration of all phases of convulsion in both maximal electroshock induced and pentylenetetrazole induced convulsion models in comparison with free drug and drug bound with nanoparticle formulations, which indicates the ability of polysorbate 80 coated nanoparticles to enhance the gabapentin concentration in the brain.

Sustained release enteric coated tablets of pantoprazole: formulation, in vitro and in vivo evaluation.

In this study, an attempt was made to deliver pantoprazole in a sustained manner using delayed release tablets. The tablets were prepared by the wet granulation method using HPMC, cassava starch and polyvinyl pyrrolidine as polymers, Avicel PH 102 (MCC) as filler and potato starch as binder. The prepared tablets were evaluated for hardness, mass variation, friability and drug content uniformity, and the results were found to comply with official standards. The prepared tablets were coated using an enteric coating polymer such as cellulose acetate phthalate, Eudragit L100 and drug coat L100 by the dip coating method. The in vitro release was studied using pH 1.2 acidic buffer and pH 6.8 phosphate buffer and the study revealed that the prepared tablets were able to sustain drug release into the intestine. The anti-ulcer activity was evaluated by a water immersion stress induced ulcer model. The enteric coated pantoprazole tablets significantly reduced ulcer formation.

Nanoparticles based on albumin: preparation, characterization and the use for 5-flurouracil delivery.

The aim of the study was to formulate and evaluate nanoparticles based on albumin to deliver 5-fluorouracil. The nanoparticles were prepared by coacervation method. The nanoparticles were characterized for particle size, surface charge, size distribution and drug loading capacity. The drug loading capacity varied from 4.22% to 19.8% (w/w). The mean particle size was 141.9 nm and surface charge was -30.3 mV. The drug loaded particles exerted a bi-phasic release pattern with an initial burst effect followed by a sustained release in pH 7.4 phosphate buffer. The drug release was first order diffusion controlled and the mechanism was Fickian. The drug loaded nanoparticles showed superior cytotoxicity when compared to the free drug.

Preparation and In vitro Investigation of Chitosan Compressed Tablets for Colon Targeting.

PURPOSE: The aim of the present study was minimizing the drug release in upper gastro intestinal tract and targeting to colon by using the principles of compression coat. METHODS: Compression coated tablets of Ibuprofen were prepared by direct compression method using chitosan (300, 250, 200 & 175 mg). Tablets were evaluated for their physicochemical properties and in vitro drug release studies. In vitro drug release studies were performed with and without rat caecal contents. RESULTS: In the rat caecal contents tablets showed enhanced drug release due to degradation of chitosan coat by colonic colonic enzymes. The in vitro release studies in pH-6.8 phosphate buffer containing 2% w/v of rat caecal contents showed the cumulative percentage release of Ibuprofen after 26h as 31.94% ±0.59, 67.89% ± 0.45 and 55.87 % ± 0.45 and 82.52 % ± 0.92 respectively. Coat thickness and amount of chitosan controls the release rate. Formulations are best fitted with Korsmeyer-Peppas kinetics and mechanism of drug release was non-Fickian. FTIR studies reveals there is no drug-polysaccharide interaction. F1 formulation was a promising system for drug targeting to colon. CONCLUSION: Based on the obtained results chitosan as a press coat could target ibuprofen to the colon.