Development of Microparticulate Sustained Release Dosage Form of Emtricitabine: An Anti-HIV Drug

Emtricitabine is a nucleotide reverse transcriptase inhibitor used for HIV infections, with oral bioavailability of 93 %. Microparticles loaded with emtricitabine were formulated through ionotropic gelation method using sodium alginate as retardant polymer and calcium chloride as cross linker. The concentration of hydroxy propyl methyl cellulose and sodium alginate were varied as 50-300 mg and 100-900 mg respectively using 3 2 factorial design. The prepared microparticles were evaluated for particle size distribution (322.66 to 553.40 mu m), percentage yield (96.68-98.33 %) drug content (92.85-95.23%) and drug entrapment efficiency (27.41 to 52.44 %). The FT-IR spectroscopic analysis indicated the minimum drug polymer interaction during preparation. The stability and uniform dispersion of drug in the polymeric matrix was confirmed by DSC and XRD studies. The in vitro release profile indicated that increase in intensity of cross linking decreased the rate of drug release, with showed significant sustained release effect of the dosage form for more than 8 h.