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Dear Colleagues,

Mucosal drug delivery is designed to direct drugs to mucosal membranes covering the respiratory tract, the eye, the female genital tract, and the gastrointestinal tract. Mucosal drug delivery is suitable for local drug administration to treat mucosal diseases, as well as for systemic drug distribution. A mucus layer covers all mucosal surfaces, protecting the underlying mucosa and representing a barrier against pathogens but also drugs or drug-carrier diffusion. Mucoadhesion is one of the strategies of mucosal delivery. Mucoadhesive drug delivery systems, due to the presence of specific polymers, adhere to the mucus layer and, therefore, prolong their retention time at the site of application/absorption, and provide a controlled rate of drug release. Moreover, other attempts have been made to optimize mucosal drug delivery, such as mucus-penetrating systems (for reducing mucus interaction), the employment of mucolytic agents (enables to alter mucus structure) and more recently self-propagating drug delivery systems or multiple absorption strategies.

The present Special Issue serves an overview of current research on Mucoadhesive and Mucosal Drug Delivery Systems, as strategies and formulative approaches to obtain the prolonged residential time at the site of application/absorption, the overcoming mucus barrier and the enhanced mucosal delivery or permeation of drugs.

Prof. Dr. Elisabetta Gavini
Dr. Giovanna Rassu
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18 pages, 9211 KiB

Open AccessArticle

Nanonization and Deformable Behavior of Fattigated Peptide Drug in Mucoadhesive Buccal Films

by Woojun Kim, Hai V. Ngo, Hy D. Nguyen, Ji-Min Park, Kye Wan Lee, Chulhun Park, Jun-Bom Park and Beom-Jin Lee

Pharmaceutics 2024, 16(4), 468; https://doi.org/10.3390/pharmaceutics16040468 - 27 Mar 2024

Viewed by 643

Abstract

This study was tasked with the design of mucoadhesive buccal films (MBFs) containing a peptide drug, leuprolide (LEU), or its diverse nanoparticles (NPs), for enhanced membrane permeability via self-assembled nanonization and deformable behavior. An LEU-oleic acid conjugate (LOC) and its self-assembled NPs (LON) were developed. Additionally, a deformable variant of LON (d-LON) was originally developed by incorporating l-α-phosphatidylcholine into LON as an edge activator. The physicochemical properties of LON and d-LON, encompassing particle size, zeta potential, and deformability index (DI), were evaluated. MBFs containing LEU, LOC, and NPs (LON, d-LON) were prepared using the solvent casting method by varying the ratio of Eudragit RLPO and hydroxypropyl methylcellulose, with propylene glycol used as a plasticizer. The optimization of MBF formulations was based on their physicochemical properties, including in vitro residence time, dissolution, and permeability. The dissolution results demonstrated that the conjugation of oleic acid to LEU exhibited a more sustained LEU release pattern by cleaving the ester bond of the conjugate, as compared to the native LEU, with reduced variability. Moreover, the LOC and its self-assembled NPs (LON, d-LON), equivalent to 1 mg LEU doses in MBF, exhibited an amorphous state and demonstrated better permeability through the nanonization process than LEU alone, regardless of membrane types. The incorporation of lauroyl-L-carnitine into the films as a permeation enhancer synergistically augmented drug permeability. Most importantly, the d-LON-loaded buccal films showed the highest permeability, due to the deformability of NPs. Overall, MBF-containing peptide NPs and permeation enhancers have the potential to replace parenteral LEU administration by improving LEU druggability and patient compliance. Full article

(This article belongs to the Special Issue Mucoadhesive and Mucosal Drug Delivery Systems, 2nd Edition)

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