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摘要
OBJECTIVE To prepare the dipalmitoylhydroxyproline nanostructured lipid carriers (DPHP-NLC) and its gel, and investigate its transdermal effect in vitro. METHODS The DPHP-NLC was prepared by high pressure homogenization, a single factor test was used to investigate the influence of the formulation process on the preparation of DPHP-NLC with the particle size, polydispersity index (PDI), Zeta potential and encapsulation efficiency as evaluation indicators, and the Box-Behnken design effect surface method was used to further screen the optimal formulation. Then, dipalmitoylhydroxyproline nanostructured lipid carriers gels(DPHP-NLC-gel) was prepared, and the in vitro transdermal permeation of DPHP-NLC and DPHP-NLC-gel was evaluated by Franze diffusion cells. RESULTS The DPHP-NLC under the optimal formulation was exhibited good dispersibility, the average particle size was (112.0±1.8) nm, PDI was (0.258±0.005), and the entrapment efficiency was (97.66±0.56)%. The results of in vitro transdermal test showed that the cumulative permeability per unit area in 24 h (Q24) of DPHP-NLC and DPHP-NLC-gel were (102.36±6.10) and (84.22±3.72) μg·cm-2 respectively, 24 h retention per unit area were (90.60±6.99) and (60.50±3.95) μg·cm-2 respectively. Q24 and 24 h retention per unit area of the DPHP suspension gel were(60.26±3.12) and (40.58±2.35) μg·cm-2 respectively. The in vitro percutaneous penetration of DPHP-NLC and DPHP-NLC-gel accorded with Higuchi equation. CONCLUSION DPHP-NLC prepared by high-pressure homogenization exhibits small particle size and high entrapment efficiency, which improves the skin permeability and retention of DPHP. ? 2022 Chinese Pharmaceutical Association.
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