A Novel Microparticle Based Formulation for Topical Delivery of FOL-005, a Small Peptide

Although many therapeutically active peptides and proteins have been developed there is a lack of topical pharmaceutical products on the market containing these sensitive molecules. The main reasons may be lack of stability and a limitation of larger molecules to penetrate into the skin. In this study we investigated the possibility to develop a peptide formulation which enables follicular permeation of peptides and passes the following criteria: 1) The formulation should be chemically and physically stable, 2) The formulation should have appealing cosmetical properties and 3) The formulation should be compatible with skin as well as sebum. The hypothesis was that increased stability of the peptide could be obtained by keeping the peptide in solid form and in a water-free environment, and that permeation into skin could be facilitated by reducing the particle size to < 10 mu m and by formulating the peptide in sebum compatible excipients. By this method a safe and a cosmetically attractive formulation, facilitating the local distribution of the model peptide FOL005 into the skin and at the same time securing chemical and physical stability, was successfully developed. (c) 2022 The Authors. Published by Elsevier Inc. on behalf of American Pharmacists Association.

Automated summary

This study aimed to develop a cosmetic formulation that enables peptide follicular permeation with chemical and physical stability and compatibility with the skin and sebum. By keeping the peptide in solid form and in a water-free environment, reducing the particle size to < 10 μm, and formulating the peptide with sebum-compatible excipients, a safe and cosmetically attractive formulation was successfully developed for the local distribution of the model peptide into the skin.