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The Vaginal-PVPA: A Vaginal Mucosa-Mimicking In Vitro Permeation Tool for Evaluation of Mucoadhesive Formulations.
Pharmaceutics. 2020 Jun 19; 12(6)P

Abstract

Drug administration to the vaginal site has gained increasing attention in past decades, highlighting the need for reliable in vitro methods to assess the performance of novel formulations. To optimize formulations destined for the vaginal site, it is important to evaluate the drug retention within the vagina as well as its permeation across the mucosa, particularly in the presence of vaginal fluids. Herewith, the vaginal-PVPA (Phospholipid Vesicle-based Permeation Assay) in vitro permeability model was validated as a tool to evaluate the permeation of the anti-inflammatory drug ibuprofen from liposomal formulations (i.e., plain and chitosan-coated liposomes). Drug permeation was assessed in the presence and absence of mucus and simulated vaginal fluid (SVF) at pH conditions mimicking both the healthy vaginal premenopausal conditions and vaginal infection/pre-puberty/post-menopause state. The permeation of ibuprofen proved to depend on the type of formulation (i.e., chitosan-coated liposomes exhibited lower drug permeation), the mucoadhesive formulation properties and pH condition. This study highlights both the importance of mucus and SVF in the vaginal model to better understand and predict the in vivo performance of formulations destined for vaginal administration, and the suitability of the vaginal-PVPA model for such investigations.

Authors+Show Affiliations

Drug Transport and Delivery Research Group, Department of Pharmacy, UiT The Arctic University of Norway, Universitetsvegen 57, 9037 Tromsø, Norway.Drug Transport and Delivery Research Group, Department of Pharmacy, UiT The Arctic University of Norway, Universitetsvegen 57, 9037 Tromsø, Norway. Dipartimento di Scienze degli Alimenti e del Farmaco, Università di Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.Drug Transport and Delivery Research Group, Department of Pharmacy, UiT The Arctic University of Norway, Universitetsvegen 57, 9037 Tromsø, Norway.Dipartimento di Scienze degli Alimenti e del Farmaco, Università di Parma, Parco Area delle Scienze 27/a, 43124 Parma, Italy.Drug Transport and Delivery Research Group, Department of Pharmacy, UiT The Arctic University of Norway, Universitetsvegen 57, 9037 Tromsø, Norway.Drug Transport and Delivery Research Group, Department of Pharmacy, UiT The Arctic University of Norway, Universitetsvegen 57, 9037 Tromsø, Norway.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

32575388

Citation

Falavigna, Margherita, et al. "The Vaginal-PVPA: a Vaginal Mucosa-Mimicking in Vitro Permeation Tool for Evaluation of Mucoadhesive Formulations." Pharmaceutics, vol. 12, no. 6, 2020.
Falavigna M, Pattacini M, Wibel R, et al. The Vaginal-PVPA: A Vaginal Mucosa-Mimicking In Vitro Permeation Tool for Evaluation of Mucoadhesive Formulations. Pharmaceutics. 2020;12(6).
Falavigna, M., Pattacini, M., Wibel, R., Sonvico, F., Škalko-Basnet, N., & Flaten, G. E. (2020). The Vaginal-PVPA: A Vaginal Mucosa-Mimicking In Vitro Permeation Tool for Evaluation of Mucoadhesive Formulations. Pharmaceutics, 12(6). https://doi.org/10.3390/pharmaceutics12060568
Falavigna M, et al. The Vaginal-PVPA: a Vaginal Mucosa-Mimicking in Vitro Permeation Tool for Evaluation of Mucoadhesive Formulations. Pharmaceutics. 2020 Jun 19;12(6) PubMed PMID: 32575388.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - The Vaginal-PVPA: A Vaginal Mucosa-Mimicking In Vitro Permeation Tool for Evaluation of Mucoadhesive Formulations. AU - Falavigna,Margherita, AU - Pattacini,Martina, AU - Wibel,Richard, AU - Sonvico,Fabio, AU - Škalko-Basnet,Natasa, AU - Flaten,Gøril Eide, Y1 - 2020/06/19/ PY - 2020/05/27/received PY - 2020/06/13/revised PY - 2020/06/17/accepted PY - 2020/6/25/entrez PY - 2020/6/25/pubmed PY - 2020/6/25/medline KW - chitosan-coated liposomes KW - in vitro studies KW - mucoadhesion KW - mucus KW - pH-dependent drug permeation KW - permeation KW - simulated vaginal fluid KW - vaginal drug administration JF - Pharmaceutics JO - Pharmaceutics VL - 12 IS - 6 N2 - Drug administration to the vaginal site has gained increasing attention in past decades, highlighting the need for reliable in vitro methods to assess the performance of novel formulations. To optimize formulations destined for the vaginal site, it is important to evaluate the drug retention within the vagina as well as its permeation across the mucosa, particularly in the presence of vaginal fluids. Herewith, the vaginal-PVPA (Phospholipid Vesicle-based Permeation Assay) in vitro permeability model was validated as a tool to evaluate the permeation of the anti-inflammatory drug ibuprofen from liposomal formulations (i.e., plain and chitosan-coated liposomes). Drug permeation was assessed in the presence and absence of mucus and simulated vaginal fluid (SVF) at pH conditions mimicking both the healthy vaginal premenopausal conditions and vaginal infection/pre-puberty/post-menopause state. The permeation of ibuprofen proved to depend on the type of formulation (i.e., chitosan-coated liposomes exhibited lower drug permeation), the mucoadhesive formulation properties and pH condition. This study highlights both the importance of mucus and SVF in the vaginal model to better understand and predict the in vivo performance of formulations destined for vaginal administration, and the suitability of the vaginal-PVPA model for such investigations. SN - 1999-4923 UR - https://www.unboundmedicine.com/medline/citation/32575388/The_Vaginal-PVPA:_A_Vaginal_Mucosa-Mimicking_In_Vitro_Permeation_Tool_for_Evaluation_of_Mucoadhesive_Formulations L2 - https://www.mdpi.com/resolver?pii=pharmaceutics12060568 DB - PRIME DP - Unbound Medicine ER -
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