The preparation and the in-vitro pharmacodynamics study of the intracapsular sustained-release preparations for the prevention of posterior capsule opacification

Abstract

Docetaxel-loaded sustained-release preparation based on 2-Hydroxyethyl methacrylate (HEMA) and Methyl methacrylate (MMA) cross-linked copolymer (P(HEMA-co-MMA)) was prepared to examine the potential use for preventing posterior capsule opacification (PCO). The preparations were prepared by polymerizing the mixture of HEMA, MMA, cross-linking agent (EGDMA), initiator (AIBN) and docetaxel. The influence factors and mechanism of drug release were studied in the experiments. FT-IR, X-RD and SEM methods were used to characterize the polymer (P(HEMA-co-MMA)) and docetaxel-loaded sustained-release preparations. Biocompatibility of P(HEMA-co-MMA) and in-vitro effect of docetaxel-loaded sustained-release preparations were also evaluated. The results showed that docetaxel could release sustainedly from these preparations prepared by cross-linking polymerization. And the release rate could be accelerated by increasing the MMA ratio or EGDMA ratio of the polymer. Release mechanism of docetaxel fitted the Higuchi model well. The results of IR and X-RD showed that only a hydrogen bond was formed between docetaxel and P(HEMA-co-MMA). Docetaxel dispersed in P(HEMA-co-MMA) in amorphous form. The elution test showed that P(HEMA-co-MMA) had good biocompatibility and the in-vitro pharmacodynamics study proved that docetaxel could release stably from the preparations and inhibit HLECs' proliferation. The docetaxel-loaded sustained-release preparations proved to be a promising therapy for preventing PCO. These results also lay a theoretical and experimental foundation for the future.