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Synthesis and Characterization of Stearic Acid-Beclomethasone Dipropionate Conjugates with the Potential for Improving Loading Capacity in Lipid-based Nanoparticles

submitted on 05.01.2021, 03:48 and posted on 11.01.2021, 06:23 by Shishuai Dang, Zhengwei Huang, Ying Huang, Xin Pan, Chuanbin Wu

Lipid-based nanoparticles (LBNs) are a new type of nanoparticulate drug delivery system, which have been gradually shown broad prospects in pulmonary drug delivery systems. However, the main disadvantage of these LBNs for inhalable drugs with limited lipophilicity is the low encapsulation capacity. Herein, this study anticipates establishing a technology platform to improve the loading capacity of low lipophilicity drugs in LBNs, for the therapy of lung diseases. A proof-of-concept was carried out using Beclomethasone dipropionate (BDP) as a model drug. BDP was conjugated with stearic acid (SA), a kind of the lipid matrix for LBN. The conjugate was characterized and the interactions between the conjugate and SA were investigated by molecular dynamics simulation. It is expected that the drug loading capacity of weak-lipophilic drugs in LBN can be increased by establishing the technology platform, and the application of LBNs in pulmonary delivery can be broadened.


Special Funds for the Cultivation of Guangdong College Students' Scientific and Technological Innovation (“Climbing Program” Special Funds) number pdjh2019a0003

National Natural Science Foundation of China

National Natural Science Foundation of China

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Sun Yat-sen University



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