Preprint Article Version 1 Preserved in Portico This version is not peer-reviewed

Development and Characterization of Thiolated Cyclodextrin-Based Nanoparticles for Topical Delivery of Minoxidil

Version 1 : Received: 9 October 2023 / Approved: 10 October 2023 / Online: 10 October 2023 (08:17:37 CEST)

A peer-reviewed article of this Preprint also exists.

Akhtar, A.; Waqas, M.K.; Mahmood, A.; Tanvir, S.; Hussain, T.; Kazi, M.; Ijaz, M.; Asim, M.H. Development and Characterization of Thiolated Cyclodextrin-Based Nanoparticles for Topical Delivery of Minoxidil. Pharmaceutics 2023, 15, 2716. Akhtar, A.; Waqas, M.K.; Mahmood, A.; Tanvir, S.; Hussain, T.; Kazi, M.; Ijaz, M.; Asim, M.H. Development and Characterization of Thiolated Cyclodextrin-Based Nanoparticles for Topical Delivery of Minoxidil. Pharmaceutics 2023, 15, 2716.

Abstract

Purpose: The aim of this research was to prepare adhesive nanoparticles for the topical application of Minoxidil (MXD). Methods: Thiolated β-CDs were prepared via conjugation of cysteamine with oxidized CDs. MXD was encapsulated within thiolated and unmodified β-CDs. Nanoparticles (Thio-NP and blank NP) were prepared by ionic gelation of CDs with chitosan. Particle size and zeta potential were measured. FTIR analyses were performed for characterization of inclusion complex. Drug dissolution studies were carried out. An in vitro adhesion study over human hair was performed. An in vivo skin irritation study was performed. Ex vivo drug uptake was evaluated by using a Franz diffusion cell. Results: Thiolated β-CDs presented 1804.68 ± 25 μmol/g thiol groups and 902.34 ± 25 μmol/g disulfide bonds. Nanoparticles displayed particle sizes within a range of 231 nm to 319 nm. The zeta potential was in the range of ̶ 8.1 to + 12.0. FTIR analyses confirmed no interaction between the excipients and drug. Delayed drug release was observed from Thio-NP. Thio-NP retained over hair surfaces for a significantly longer time. Similarly, drug retention was significantly improved. Thio-NP displayed no irritation over rabbit skin. Conclusion: Owing to the above results, nanoparticles developed with MXD-loaded thiolated β-CDs might be a potential drug delivery system for topical scalp diseases.

Keywords

thiomers; cyclodextrin; hair keratin; minoxidil; hair adhesion

Subject

Chemistry and Materials Science, Biomaterials

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