Baicalein Loaded Crown Ether-mPEG-PLGA Micelle Drug Delivery System for Increased Breast Cancer Treatment: Preparation, Characterization, In-Vitro and In-Vivo Evaluations

Abstract

Due to low aqueous solubility and poor bioavailability of the flavone baicalein (BIC), a nano-micelle of delivery system was developed. Preparation of BIC-loaded crown ether-mPEG-PLGA micelle (BCPP-M) was performed via thin-film hydration method. Characterization of micellar excipients was accomplished with 1H NMR, while evaluation of the optimal BCPP-M formulation was appropriately carried out through zeta potential (ZP), size of particles (PS), efficiency of encapsulation (EE) and capacity of drug loading (DL). We evaluated BIC release In-Vitro and profile of In-Vivo pharmacokinetics. Evaluation of the anti-breast cancer property of BCPP-M using MCP-7 cells cytotoxicity and mice model was performed. Particles of BCPP-M were homogenously and spherically shaped with smaller average PS, coupled with higher EE and DL, good stability and polydispersity index (PDI). The accumulative release of BCPP-M was obviously higher than free-BIC. Significantly, oral biological availability of BCPP-M was improved comparable to free BIC. Besides, half maximum inhibitory concentration (IC50) of BCPP-M in MCP-7 cells was lower than free-BIC. Animal experiments also showed targeting, long circulation and antitumor potential of BCPP-M. Successful incorporation of BIC into long-acting and targeting micellar system could have enhanced solubility in aqueous media, oral In-Vivo availability and antitumor property of BIC.