Lipids-based nanostructured lipid carriers (NLCs) for improved oral bioavailability of sirolimus

Qin YuDepartment of Pharmaceutics, School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA, Shanghai, China and

Xiongwei HuDepartment of Pharmaceutics, School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA, Shanghai, China and

Yuhua MaDepartment of Pharmaceutics, School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA, Shanghai, China and

Yunchang XieDepartment of Pharmaceutics, School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA, Shanghai, China and

Yi LuDepartment of Pharmaceutics, School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA, Shanghai, China and

Jianping QiDepartment of Pharmaceutics, School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA, Shanghai, China and

Li XiangDepartment of Pharmacy, Shanghai Xuhui Dahua Hospital, Shanghai, China

Fengqian LiDepartment of Pharmacy, Shanghai Xuhui Dahua Hospital, Shanghai, ChinaCorrespondence[email protected]

Wei WuDepartment of Pharmaceutics, School of Pharmacy, Fudan University, Key Laboratory of Smart Drug Delivery of MOE And PLA, Shanghai, China and Correspondence[email protected]

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Abstract

The main purpose of this study was to improve the oral bioavailability of sirolimus (SRL), a poorly water-soluble immunosuppressant, by encapsulating into lipids-based nanostructured lipid carriers (NLCs). SRL-loaded NLCs (SRL-NLCs) were prepared by a high-pressure homogenization method with glycerol distearates (PRECIROL ATO-5) as the solid lipid, oleic acid as the liquid lipids, and Tween 80 as the emulsifier. The SRL-NLCs prepared under optimum conditions was spherical in shape with a mean particle size of about 108.3 nm and an entrapment efficiency of 99.81%. In vitro release of SRL-NLCs was very slow, about 2.15% at 12 h, while in vitro lipolysis test showed fast digestion of the NLCs within 1 h. Relative oral bioavailability of SRL-NLCs in Beagle dogs was 1.81-folds that of the commercial nanocrystalline sirolimus tablets Rapamune®. In conclusion, the NLCs show potential to improve the oral bioavailability of SRL.

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Lipids-based nanostructured lipid carriers (NLCs) for improved oral bioavailability of sirolimus

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Lipids-based nanostructured lipid carriers (NLCs) for improved oral bioavailability of sirolimus

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