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Preformulation and stability in biological fluids of the retrocyclin RC-101, a potential anti-HIV topical microbicide

Sassi, AB and Bunge, KE and Hood, BL and Conrads, TP and Cole, AM and Gupta, P and Rohan, LC (2011) Preformulation and stability in biological fluids of the retrocyclin RC-101, a potential anti-HIV topical microbicide. AIDS Research and Therapy, 8.

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Background: RC-101, a cationic peptide retrocyclin analog, has in vitro activity against HIV-1. Peptide drugs are commonly prone to conformational changes, oxidation and hydrolysis when exposed to excipients in a formulation or biological fluids in the body, this can affect product efficacy. We aimed to investigate RC-101 stability under several conditions including the presence of human vaginal fluids (HVF), enabling the efficient design of a safe and effective microbicide product. Stability studies (temperature, pH, and oxidation) were performed by HPLC, Circular Dichroism, and Mass Spectrometry (LC-MS/MS). Additionally, the effect of HVF on formulated RC-101 was evaluated with fluids collected from healthy volunteers, or from subjects with bacterial vaginosis (BV). RC-101 was monitored by LC-MS/MS for up to 72 h.Results: RC-101 was stable at pH 3, 4, and 7, at 25 and 37°C. High concentrations of hydrogen peroxide resulted in less than 10% RC-101 reduction over 24 h. RC-101 was detected 48 h after incubation with normal HVF; however, not following incubation with HVF from BV subjects.Conclusions: Our results emphasize the importance of preformulation evaluations and highlight the impact of HVF on microbicide product stability and efficacy. RC-101 was stable in normal HVF for at least 48 h, indicating that it is a promising candidate for microbicide product development. However, RC-101 stability appears compromised in individuals with BV, requiring more advanced formulation strategies for stabilization in this environment. © 2011 Sassi et al; licensee BioMed Central Ltd.


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Item Type: Article
Status: Published
CreatorsEmailPitt UsernameORCID
Sassi, AB
Bunge, KE
Hood, BL
Conrads, TPtpc7@pitt.eduTPC7
Cole, AM
Gupta, Ppgupta1@pitt.eduPGUPTA1
Rohan, LC
Centers: Other Centers, Institutes, Offices, or Units > Magee-Women's Research Institute
Other Centers, Institutes, Offices, or Units > Pittsburgh Cancer Institute
Date: 29 July 2011
Date Type: Publication
Journal or Publication Title: AIDS Research and Therapy
Volume: 8
DOI or Unique Handle: 10.1186/1742-6405-8-27
Schools and Programs: School of Medicine > Infectious Diseases and Microbiology
School of Medicine > Obstetrics, Gynecology, and Reproductive Sciences
School of Medicine > Pharmacology and Chemical Biology
School of Pharmacy > Pharmaceutical Sciences
Refereed: Yes
Date Deposited: 31 Oct 2016 16:37
Last Modified: 02 Feb 2019 16:58


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