1. Development of a mucoadhesive delivery system for control release of doxepin with application in vaginal pain relief associated with gynecological surgery.
- Author
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Sanz R, Clares B, Mallandrich M, Suñer-Carbó J, Montes MJ, and Calpena AC
- Subjects
- Adhesiveness, Administration, Intravaginal, Analgesics chemistry, Animals, Doxepin chemistry, Drug Liberation, Drug Stability, Female, Mucous Membrane chemistry, Pain drug therapy, Rheology, Swine, Vagina, Viscosity, Analgesics administration & dosage, Doxepin administration & dosage, Drug Delivery Systems
- Abstract
The main purpose of this study was to develop a semisolid mucoadhesive formulation for the non-invasive vaginal administration of doxepin (DOX) for relief of pain derived from the scarring process after surgery. An orafix
® platform loading DOX was tested for adequate stability, rheology and vaginal mucoadhesion capacity. The formulation exhibited appropriate pH and was microbiologically stable. The rheological studies confirmed its pseudoplastic and thixotropic nature with prevalence of the elastic behavior component over the viscous one. Appropriate syringeability and spreadability results were also confirmed. Different experiments showed adequate mucoadhesion capacity even in the presence of simulated vaginal fluid. Finally, DOX release, permeation and retention in vaginal mucosa studies were also accomplished with promising results. DOX release kinetics followed the modified Higuchi model and the permeation studies did not render such high values as to suggest potential systemic absorption which could lead to undesirable systemic side effects. Therefore, we can hypostatize that the proposed formulation may assist to fill in the therapeutic gap regarding pure pain relief at local level in vagina., (Copyright © 2017 Elsevier B.V. All rights reserved.)- Published
- 2018
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