Preparation and characterization of 7-ethyl-10-hydroxycamptothecin-loaded hypomicron of amphiphilic block copolymer / 药学学报

ABSTRACT

Methoxypolyethylene glycol-poly lactic acid (PELA) was synthesized by ring-opening copolymerization of lactide in the presence of mPEG and its structure was characterized by 1H NMR. The novel hypomicrons were prepared by solution-casting method using PELA block copolymer as a matrix and 7-ethyl-10-hydroxycamptothecin (SN-38) as an antitumor agent. The morphology, size and size distribution, drug loading, entrapment efficiency, and release characteristics in vitro of the SN-38 loaded hypomicrons were studied. The results showed that the obtained hypomicrons showed spherical shape with the core-shell structure, the sizes are in the range of 157-238 nm, and the drug loading content varied from 1.35%-3.58% depending on the copolymer composition and the SN-38 fed amount. The in vitro release behavior in phosphate-buffered saline, pH 7.4, exhibited a sustaining release manner and was affected by the copolymer composition. The drug-loaded amount and entrapment efficiency decreased with increasing the molecular weight of the copolymer. With the increasing of the SN-38 fed amount, the drug-loaded amount and the size of hypomicrons increased, the entrapment efficiency decreased. The SN-38 hypomicrons increased the solubility of SN-38 in water and were valuable for the development of the novel dosage form of SN-38.