Etravirine

Etravirine is a non-neucleoside reverse transcriptase inhibitor (NNRTI) used in the treatment of HIV. One of the major problems with the Etravirine is its low solubility, which results into poor bioavailability after oral administration. Therefore, solid dispersions (SDs) of Etravirine were prepared by two methods, Hot-melt extrusion and Spray drying technique using various carriers like Polyvinyl Caprolactam-Polyvinyl Acetate-Polyethylene Glycol Graft Copolymer (Soluplus), Hypromellose 2.5 cPs, PEG 6000, Amino Methacrylate Copolymer (Eudragit EPO) & Copovidone (Kollidon VA64) and Povidone (Kollidon 30) to increase its aqueous solubility. Faster and high drug release was found in the SDs prepared by hot melt extrusion (HME) with soluplus in the ratio of 1:3 as compared with spray drying technique (SDT) using drug substance, Soluplus and Microcrystalline cellulose (Avicel PH105) in the ratio of 1:2:0.5. There is 3 fold increases in the solubility of Etravirine prepared by HME & SDT compared with pure drug substance. HM3 and SDT4 are finalized as optimized formulations prepared by HME & SDT based on their solubility, drug substance content and in vitro drug dissolution studies. FT-IR, DSC and XRD of SDs by HME & SDT showed a change in crystal structure toward an amorphous form of Etravirine. The obtained results suggested that developed Etravirine SDs by HME & SDT has potential for oral delivery and might be an efficacious approach for enhancing the therapeutic potential of Etravirine.