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Development of a Vaginal Film for Delivering a Sperm-Deactivating Non-Hormonal Contraceptive Candidate, Lupeol.

Chiang, YunShan (2020) Development of a Vaginal Film for Delivering a Sperm-Deactivating Non-Hormonal Contraceptive Candidate, Lupeol. Master's Thesis, University of Pittsburgh. (Unpublished)

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To date, there are only limited nonhormonal contraceptive options available. Therefore, development of nonhormonal contraceptive products represents a gap in female reproductive healthcare needs. Lupeol, a triterpenoid found in a number of fruits and vegetables, is currently being evaluated by YourChoice Therapeutics (CA, USA) as a potential novel nonhormonal contraceptive agent. Sperm hyperactivation is required for fertilization to occur as it facilitates the sperm cells’ ability to migrate in the high viscosity fluids within the female genital tract and allows for penetration of the cumulus cells surrounding the egg. Abhydrolase domain-containing protein 2 (ABHD2) is a serine hydrolase enzyme expressed in human spermatozoa which is essential for sperm hyperactivation. Lupeol modulates ABHD2 i.e. it blocks progesterone from binding to ABHD2, which is essential for sperm hyperactivation to occur. Therefore, it can deactivate sperm mobility and avoid egg fertilization, thereby preventing pregnancy. To facilitate its use as a contraceptive product, lupeol must be formulated into a vaginal dosage form which women can utilize in the context of sexual intercourse. Vaginal films have been identified as an acceptable vaginal dosing option. Given its extreme hydrophobicity, formulation of lupeol is challenging. This thesis will describe the pre-formulation studies of lupeol, including the development of a critical analytical method and cytotoxicity study of lupeol in VK2 cell line, and the formulation development based on a polymeric thin film platform. The prototype film product developed was designed to rapidly release lupeol in the vaginal compartment using a hydroxyethyl cellulose based polymeric thin film. The physicochemical properties of the lupeol immediate-release vaginal film were characterized and were followed by a short-term stability to evaluate drug content and physical properties, such as the water content, disintegration time, puncture strength and contact angle. Additionally, optimization of the formulation was proposed to improve the physical properties of the film prototype. Development of the novel nonhormonal contraceptive drug candidate, lupeol, into a coitally-dependent product is essential for its advancement to future evaluation in women.


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Item Type: University of Pittsburgh ETD
Status: Unpublished
CreatorsEmailPitt UsernameORCID
Chiang, YunShanchiangyunshan@gmail.comyuc114
ETD Committee:
TitleMemberEmail AddressPitt UsernameORCID
Committee ChairRohan,
Committee MemberPatel, Sravanpatels10@mwri.magee.edusrp75
Committee MemberSant, Vinayakvis45@pitt.eduvis45
Date: 24 April 2020
Date Type: Publication
Defense Date: 2 April 2020
Approval Date: 24 April 2020
Submission Date: 23 April 2020
Access Restriction: 2 year -- Restrict access to University of Pittsburgh for a period of 2 years.
Number of Pages: 116
Institution: University of Pittsburgh
Schools and Programs: School of Pharmacy > Pharmaceutical Sciences
Degree: MS - Master of Science
Thesis Type: Master's Thesis
Refereed: Yes
Uncontrolled Keywords: Vaginal film formulation, female-controlled contraceptive, non-hormonal contraceptive, triterpenoids, CatSper, sperm hyperactivation, lupeol.
Date Deposited: 24 Apr 2020 14:26
Last Modified: 24 Apr 2022 05:15


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