Description of the intrafollicular delivery of large molecular weight molecules to follicles of human scalp skin in vitro

作者: Linda M. Lieb , Andrew P. Liimatta , Robert N. Bryan , Bob D. Brown , Gerald G. Krueger

DOI: 10.1021/JS9700053

关键词: StereochemistryDosage formFluoresceinLiberationDrug carrierFluorescence microscopeBiophysicsLiposomeRoot sheathHair follicleChemistry

摘要: The objective of this study was to ascertain the elements that govern intrafollicular delivery large molecules follicles human scalp skin in vitro. experiments were designed assess disposition drug as a function size, charge, and formulation. First, fluorescein covalently linked antisense oligonucleotides rhodamine-conjugated dextrans topically applied fresh position follicle qualitatively determined by examining histologic sections hair-bearing taken parallel surface at various depths dissected hair via fluorescent microscopy. Using radiolabeled we demonstrated these cross can also be used quantitatively localize Experimental results showed cationic lipid-based formulations enhanced within follicle. qualitative analysis illustrated directed permeation along junction internal external root sheath. charged, lower molecular weight (MW) permeated into all components follicle, including shaft. higher MW confined follicular structures immediately surrounding demonstration quantitation approximately 0.5% dose delivered bulbs deeper strata 24 h single application. We conclude agents relatively MW, properly formulated vehicles; have potential reach pharmacologically active concentrations bulb. It should noted takes place

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