Preactivated hyaluronic acid: A potential mucoadhesive polymer for vaginal delivery

[Display omitted] The objective of this study was to develop mucoadhesive polymeric excipients for vaginal drug delivery systems. Hyaluronic acid was thiolated and subsequently preactivated with 6-mercaptonicotinamide (HA-CYS–MNA) to enhance stability and mucoadhesive properties on vaginal mucosa. A...

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Bibliographic Details
Published in:International journal of pharmaceutics 2015-01, Vol.478 (1), p.383-389
Main Authors: Nowak, Jessika, Laffleur, Flavia, Bernkop-Schnürch, Andreas
Format: Article
Language:English
Subjects:
Adhesiveness
Administration, Intravaginal
Animals
Caco-2 Cells
Cattle
Cell Survival - drug effects
Drug Delivery Systems
Excipients - chemistry
Female
Humans
Hyaluronic acid
Hyaluronic Acid - administration & dosage
Hyaluronic Acid - chemistry
Mucoadhesion
Mucous Membrane - chemistry
Niacinamide - administration & dosage
Niacinamide - analogs & derivatives
Niacinamide - chemistry
Polymers - chemistry
Preactivated thiomers
Sulfhydryl Compounds - administration & dosage
Sulfhydryl Compounds - chemistry
Tablets
Tensile Strength
Thiomers
Vaginal delivery
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Summary:[Display omitted] The objective of this study was to develop mucoadhesive polymeric excipients for vaginal drug delivery systems. Hyaluronic acid was thiolated and subsequently preactivated with 6-mercaptonicotinamide (HA-CYS–MNA) to enhance stability and mucoadhesive properties on vaginal mucosa. After determination of the thiol group content, disintegration studies and in vitro mucoadhesion studies (rotating cylinder and tensile) were performed. Furthermore, swelling behavior and cytotoxicity studies were performed in comparison with corresponding polymers. Both, disintegration and in vitro mucoadhesive studies revealed that modifying HA-CYS with MNA resulted in higher stability (3.6-fold prolonged disintegration time compared to unmodified hyaluronic acid) and prolonged mucoadhesion time. MTT assay and LDH revealed no toxicity for the polymeric excipients and safe for their use. Disintegration and swelling results conducted more pronounced stability of the preactivated thiomers compared to corresponding unmodified ones. According to these results preactivated hyaluronic acid might be a useful tool for vaginal delivery systems.
ISSN:0378-5173
1873-3476
DOI:10.1016/j.ijpharm.2014.11.048