Development and Evaluation of Polymeric Micelle Containing Tablet Formulation for Poorly Water Soluble Drug: Tamoxifen Citrate.

In this study poly(ethylene glycol)-block-poly(propylene glycol)-block-poly(ethylene glycol) triblock copolymer, which has been approved by FDA for oral application was used to benefit its micellar solubilization effect. Self-assembled micelles were prepared for the delivery of TMX and this way TMX solubility was increased approximately 60 times. TMX treated cells showed 38.06 ± 1.5% viability at 50 μM concentration for 24h; 66.71 ± 11.6% viability at 25 μM concentration for 48h, at the same conditions TMX loaded micelles exhibited 24.994 ± 0.25% and 43.36 ± 4.37% cell viability respectively (P < 0.05). These results showed that, encapsulation of TMX into PEG-PPG-PEG micelles facilitated the cellular uptake, which led to an increased cytotoxicity in MCF-7 cancer cells. Tablet formulation containing lyophilized TMX loaded micelles was showed an improved dissolution than commercial TMX tablet(Tamoxifen® Teva). It can be reasonably expected that the obtained drug dissolution rate and increased cytotoxicity to tumor cells will result in an increase of TMX bioavailability and tolerability associated with an important dose reduction and decreased side effects. PMID: 32893676 [PubMed - as supplied by publisher]
Source: Drug Development and Industrial Pharmacy - Category: Drugs & Pharmacology Tags: Drug Dev Ind Pharm Source Type: research