Objective: Lamivudine (LVD) is a nucleoside reverse transcriptase inhibitor originally developed as an antiretroviral drug and primarily used in the treatment of most common chronic disease of the planet, acquired immune deficiency syndrome and hepatitis B. The main objective of the study is to develop controlled drug delivery system to increase the efficacy of antiretroviral drug, LVD against human immunodeficiency virus infections. Methods:The microencapsulation of LVD in gelatin microspheres was carried out by cross-linking process with glutaraldehyde saturated toluene using ionic-gelation method. The prepared microspheres were evaluated for particle size analysis, % yield value, % drug content, drug entrapment efficiency, scanning electron microscopy for surface morphology, swelling index, accelerated stability studies, Fourier transform infrared radiation spectroscopy (FT-IR) and differential scanning calorimetry (DSC) for polymer drug compatibility, in vitro dissolution efficiency and release kinetic studies. Results:The obtained microspheres showed very smooth surface and exhibited regular spherical geometry due to higher crosslinking density. FT-IR and DSC revealed the absence of drug polymer interactions. The percentage yield, entrapment efficiency and drug content for F6 LVD microspheres was found to be 79.31%, 65.55% and 96.25% respectively. The particle size was ranged from 34.61% to 51.45 µm sizes and in vitro release profile showed that cross-linking density of gelatin microspheres effectively controlled the release of LVD. Conclusion:The findings of our investigation demonstrated that F6 of gelatin-LVD microspheres had good controlled release profile with maximum entrapment efficiency and prolonged drug release for 24 hrs or longer and this formulation would be capable of overcoming the drawbacks and limitations of LVD conventional dosage forms.

Objectives: The present objective for the study was to prepare proliposomal gel bearing an antifungal agent, fluconazole (FLZ) intended for topical application.Methods: Various proliposome formulations were prepared using thin-film hydration technique by varying the lipid phase composition (phosphatidylcholine/cholesterol). Proliposome formulations were characterized for vesicle size, vesicle size distribution, vesicle morphology, drug content, entrapment efficiency, percentage yield value, storage stability analysis, Fourier-transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), in vitro diffusion study, release kinetic studies, and antifungal activity. Topical proliposomal gels were prepared by incorporation of lyophilized proliposome into a structured vehicle carbopol 934 (2.5%).Results: A spherical shape of reconstituted FLZ liposome with an average vesicle about 5–8 μm was observed in photomicrographs. The percentage entrapment of drug was increased with increase in phospholipid composition in the range of 55.13–69.61%. The FTIR and DSC studies showed no possible drug-excipient interaction. Proliposomal gel showed the prolonged release of FLZ than the lyophilized liposomes. The release kinetic values of regression coefficients confirmed the diffusion-dependent release of the drug. Stability studies indicated that product is stable and should be stored at low temperature.Conclusion: The proposed FLZ proliposomal gel showed sustained release with enhanced antifungal activity implicating its potential in effective transdermal delivery for the topical pharmacotherapy.