DEVELOPMENT, EVALUATION AND TARGETING OF STAVUDINE LOADED SERUM ALBUMIN POLYMER BASED NANOCARRIERS TO HIV RESERVOIRS

Objective: Stavudine is an antiretroviral drug that is part of the nucleoside reverse transcriptase inhibitor (NRTIs) family, which is used to delay the progression of HIV infection. The present investigation involves the development and evaluates stavudine loaded nanocarriers using natural polymer bovine serum albumin (BSA). Methods: The desolvation technique was used to prepare nanoparticles and coated with 1% v/v polysorbate 80 to improve the targeting of drugs to the organs (HIV reservoirs). Biodistribution studies were also investigated for the best formulation to determine the targeting efficiency of nanocarriers loaded stavudine and compared with pure compound. Results: The formulated nanocarriers have shown mean particle size below 300 nm, zeta potential in the range of -16.5 Mv, encapsulation efficiency in the range of 50.10 to 73.7%, drug loading in the range of 14.73 to73.84%. Cumulative % drug release was in the range of 24.72 to 71.20% and release kinetics studies showed that the mechanism of drug release was controlled simultaneously by diffusion and erosion of the matrix type formulations. The stability studies over a period of three months confirmed the stability of BSA nanoparticles. Biodistribution studies demonstrated that nanoparticles coated with 1% v/v polysorbate 80 were able to reach the HIV reservoirs in an amount higher than that of uncoated stavudine nanoparticles or pure drug itself. Conclusion: The method adopted is simple and the biodistribution studies demonstrated that nanoparticles coated with 1% polysorbate 80 were able to reach the selected organs in an amount higher than that of uncoated stavudine nanoparticles or pure drug itself

TRANSDERMAL DELIVERY OF AN EFFECTIVE NONSTEROIDAL ANTI-INFLAMMATORY DRUGS FOR PAIN MANAGEMENT IN ARTHRITIS

Objective: The current research work has been carried out with the aim to develop a transdermal gel formulation of fenoprofen (a nonsteroidal anti-inflammatory drug used to treat pain associated in arthritis) which would overcome the gastrointestinal-related problems associated with oral administration of the drug. The present study aims at formulating transdermal gels using different concentrations of Carbopol, hydroxypropyl methylcellulose (HPMC), sodium alginate, and guar gum. Methods: The formulated gels were subjected for various evaluation tests such as clarity, homogeneity, viscosity, drug content, pH, spreadability, and in vitro permeation studies. Drug–polymer interaction was studied by Fourier transmission infrared (FTIR) and differential scanning calorimetry (DSC). The in vitro permeation studies were performed in phosphate buffer 7.4 using Franz diffusion cell. Results: The FT-IR and DSC studies showed no chemical interaction between drug and polymers used. All the formulated gels showed acceptable physical properties with respect to clarity, homogeneity, viscosity, drug content, pH, and spreadability. Among all the gel formulations, Carbopol gels containing fenoprofen showed good drug release compared to HPMC, sodium alginate, and guar gum. Optimized formulation was further subjected to kinetic studies which showed Higuchi model of drug release. The same formulation showed significant anti-inflammatory and analgesic activity, tested in Wistar albino rats. No signs of erythema, edema, flushing, and papules were observed when skin irritation test was performed. Stability studies under accelerated condition showed satisfactory results for the optimized formulation. Conclusions: Thus, it was concluded from the results that the optimized formulation showed controlled and slow drug delivery. Animal studies were significant at p<0.05 and 0.001. The selected formulation was stable at various ambient temperatures