Harmine loaded Galactosylated Pluronic F68-Gelucire 44/14 mixed micelles for liver targeting.

Harmine loaded Galactosylated Pluronic F68-Gelucire 44/14 mixed micelles for liver targeting. Drug Dev Ind Pharm. 2019 May 16;:1-29 Authors: Kushwaha JP, Baidya D, Patil S Abstract Harmine (HM), a phytoconstituent has wide range of pharmacological activities including antimicrobial, antifungal, antioxidative and anticancer. HM has shown promising anticancer activity against liver cancer cells. However, poor aqueous solubility, multidrug pump P-gp efflux, extensive in vivo metabolism and rapid elimination due to glucuronidation/sulfation limits clinical utility of HM. In order to overcome the drawbacks of HM, the current work reports preparation of HM loaded galactosylated pluronic F-68 (PF68)-Gelucire® 44/14(GL44) mixed micelles (HM-MM). 32 Factorial design was used to investigate the effect of formulation variables on formation HM loaded mixed micelles. Solvent evaporation method was used for preparation of HM-MM. The optimized HM-MM was evaluated for size, percent drug entrapped (EE), in vitro HM release, oral bioavailability and biodistribution in rats. HM-MM with an average size 277.5 ± 3.24nm had an EE of 86.5 ± 1.51% w/w. HM-MM released HM in a controlled manner. Additionally, HM-MM showed significant enhancement in oral bioavailability (around 6-folds) of HM when compared to HM alone. Further, HM-MM showed around 7 fold higher amount of HM in the liver when compared to HM alone revealing efficient drug ...
Source: Drug Development and Industrial Pharmacy - Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research

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Source: International Journal of Oral and Maxillofacial Surgery - Category: ENT & OMF Authors: Tags: Research Paper Source Type: research
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