A molecular mechanism investigation of the transdermal/topical absorption classification system on the basis of drug skin permeation and skin retention

透皮 渗透 化学 色谱法 吸收(声学) 药品 赋形剂 药理学 材料科学 生物化学 医学 复合材料
作者
Qi Tian,Peng Quan,Liang Fang,Hui Xu,Chao Liu
出处
期刊:International Journal of Pharmaceutics [Elsevier BV]
卷期号:608: 121082-121082 被引量:35
标识
DOI:10.1016/j.ijpharm.2021.121082
摘要

A transdermal/topical absorption classification system for the characterization of the systemic or local delivery of drugs is the theoretical basis for the design and evaluation of transdermal/topical formulations. A classification system was established on the basis of the in vitro and in vivo skin permeation/retention behaviors of 12 model drugs. Drug skin penetration/retention exhibited a significant correlation with physicochemical parameters (log KO/W, molecular weight, polar surface area, and polarizability). Four representative model drugs were selected to clarify the molecular mechanisms of drug skin permeation/retention behaviors. The excellent lipid-disrupting effect and enhanced partitioning exhibited by propranolol (high permeation–high retention) and zolmitriptan (high permeation-low retention) via the formation of moderate H-bonds with skin lipids were proven by ATR–FTIR (ΔνasCH2 > 2 cm−1), Raman spectra (ΔLPP, SPP > 0.2 nm), and X-ray scattering (lipid crystallization) and were supported by 13C NMR results. The low lipid miscibility of zolmitriptan (ΔHzolmitriptan-lipid = 126.92 J/g) caused the low skin retention of this drug. High polarizabiltiy (α = 38.5 × 10−24 cm3) and low H-bond forming capability (EH-bond = 0 kcal/mol) restricted terbinafine (low permeation–high retention) in terms of partitioning (kD-SC = 0.09). Diclofenac (low permeation–low retention) stabilized skin lipids through the formation of strong H-bonds and exhibited excessive drug–lipid miscibility (ΔHdiclofenac-skin = −128.73 J/g), thus restricting its skin absorption. This classification system reflects the most essential drug skin absorption characteristics and provides a theoretical basis for the design of transdermal/topical formulations.
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