Design of antiretroviral drug-polymeric nanoparticles laden buccal films for chronic HIV therapy in paediatrics

Anti-HIV drug Lamivudine exhibit shorter half-life (2 h) and poor bioavailability (62% in paediatric patients), multiple dosing is required. To overcome the limitations, nanoparticles loaded buccal film was developed for prolonged drug release and improved efficiency. Nanoprecipitated Lamivudine-Eudragit E100 polymeric nanoparticles exhibited average particle size of 338 nm with polydispersity index 0.315. Buccal films prepared by solvent casting technique using sodium carboxy methyl cellulose and polyvinyl pyrrolidone (3:2) loaded with the nanoparticles showed initial drug release of 49% followed by sustained release to reach the maximum of 93% at the end of 8 h. Encapsulation of drug in nanoparticles and the film was confirmed through scanning electron microscopy, thermal and crystal characterization. Sustained drug release through Fickian diffusion mechanism from the matrix system was confirmed. The optimized formulation could be used to enhance therapeutic effect at reduced dose and side effects, especially for the paediatric anti-HIV therapy.

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