Next Article in Journal
Quantitative Prediction of Human Pharmacokinetics and Pharmacodynamics of CKD519, a Potent Inhibitor of Cholesteryl Ester Transfer Protein (CETP)
Previous Article in Journal
Towards Printed Pediatric Medicines in Hospital Pharmacies: Comparison of 2D and 3D-Printed Orodispersible Warfarin Films with Conventional Oral Powders in Unit Dose Sachets
Previous Article in Special Issue
Smart Freeze-Dried Bigels for the Prevention of the Sexual Transmission of HIV by Accelerating the Vaginal Release of Tenofovir during Intercourse
Article Menu
Issue 7 (July) cover image

Export Article

Open AccessArticle

17-α Hydroxyprogesterone Nanoemulsifying Preconcentrate-Loaded Vaginal Tablet: A Novel Non-Invasive Approach for the Prevention of Preterm Birth

1
Pharmaceutical Sciences, St. John’s University, Queens, NY 11439, USA
2
Pathology and Obstetrics and Gynecology and Women’s Health, Montefiore Medical Center/Albert Einstein College of Medicine, Bronx, NY 10461, USA
*
Authors to whom correspondence should be addressed.
Pharmaceutics 2019, 11(7), 335; https://doi.org/10.3390/pharmaceutics11070335
Received: 9 May 2019 / Revised: 9 July 2019 / Accepted: 11 July 2019 / Published: 14 July 2019
(This article belongs to the Special Issue Vaginal Drug Delivery for Local and Systemic Applications)
  |  
PDF [2326 KB, uploaded 16 July 2019]
  |  

Abstract

Preterm birth (PTB) is a major cause of infant mortality in the United States and around the globe. Makena®—once-a-week intramuscular injection of 17-α Hydroxyprogesterone caproate (17P)—is the only FDA approved treatment for the prevention of PTB. Invasive delivery of 17P requires hospitalization and expert personnel for injection. Vaginal delivery of 17P would be preferable, because of high patient compliance, reduced systemic exposure, fewer side effects, and no need for hospitalization. The objective of the present study was to prepare and evaluate a self-nanoemulsifying vaginal tablet of 17P. A solid self-nanoemulsifying preconcentrate (S-SNEDDS) of 17P and dimethylacetamide (DMA) was developed using medium chain triglycerides, a non- immunogenic surfactant, and co-processed excipient (PVA-F100). The tablet prepared was characterized for emulsification time, particle size, solid state properties, and drug release. The formulation showed >50% inhibition of TNF-α release from LPS-stimulated RAW 264.7 cells. Importantly, there were significant differences in rates of PTB and average time to delivery between control and vaginal 17P-treated groups in LPS-stimulated timed pregnant E15.5 mice. Considering the lacuna of therapeutic approaches in this area, vaginal delivery of 17P for the prevention of preterm birth has significant clinical relevance. View Full-Text
Keywords: 17-α hydroxyprogesterone caproate; preterm birth; self-nanoemulsifying system; preterm labor; vaginal delivery; nanoparticle; vaginal tablet 17-α hydroxyprogesterone caproate; preterm birth; self-nanoemulsifying system; preterm labor; vaginal delivery; nanoparticle; vaginal tablet
Figures

Figure 1

This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited (CC BY 4.0).
SciFeed

Share & Cite This Article

MDPI and ACS Style

Patki, M.; Giusto, K.; Gorasiya, S.; Reznik, S.E.; Patel, K. 17-α Hydroxyprogesterone Nanoemulsifying Preconcentrate-Loaded Vaginal Tablet: A Novel Non-Invasive Approach for the Prevention of Preterm Birth. Pharmaceutics 2019, 11, 335.

Show more citation formats Show less citations formats

Note that from the first issue of 2016, MDPI journals use article numbers instead of page numbers. See further details here.

Related Articles

Article Metrics

Article Access Statistics

1

Comments

[Return to top]
Pharmaceutics EISSN 1999-4923 Published by MDPI AG, Basel, Switzerland RSS E-Mail Table of Contents Alert
Back to Top