Lipid‐enveloped PLGA as a hybrid carrier for sustained delivering camptothecin in ovarian cancer

Abstract

Camptothecin (CPT) is plant alkaloid exhibiting in a wide range of solid tumours. However, CPT was instability at physiological pH conditions, the lactone moieties easily hydrolysed makes systemic toxicity risky. Moreover, the water insolubility of CPT was obstructed in clinical development. The aim of the study was to utilise nontoxic and biodegradable poly(D,L‐lactic‐co‐glycolic acid) (PLGA) incorporated lipid as a hybrid nanoparticle (lipid‐PLGA NPs) for delivery of CPT. Lipid‐PLGA NPs were produced by a nano‐precipitation technique. The optimal formulation was presented that particles of which were 43 nm in diameter, with a polydispersity index of 0.3 which indicated a smaller and well‐distributed pattern. Moreover, a high capacity of ∼95% entrapment efficiency was achieved. An in vitro release study showed that non‐formulated CPT with a lag time of ∼0 h, demonstrated an obvious burst effect; in contrast, sustained released and a lag time delay were clearly observed in lipid‐PLGA NPs. The cytotoxicity study confirmed that human ovarian cancer cells (ES‐2) were inhibited by lipid‐PLGA NPs. CPT was successful entrapped in lipid‐PLGA NPs which achieved smaller size and well distribution. Lipid‐PLGA NPs resolve the water insolubility and produced a sustained, slow‐release pattern of CPT and controlled the cytotoxicity toward ES‐2.