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Construction of Lipid-Drug Conjugates for Beclomethasone Dipropionate
1 , * 2 , * 3
1  School of Pharmaceutical Science, Sun Yat-sen University
2  College of Pharmacy, Jinan University
3  School of Pharmaceutical Sciences, Sun Yat-sen University
Academic Editor: Julio A. Seijas


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.

Keywords: Lipid-based nanoparticles; beclomethasone dipropionate; stearic acid; pulmonary administration