Jul 212016

Simi Gunaseelan Ph.D  Author

Assistant Professor of Pharmaceutical Sciences, The University of Texas at Tyler, TEXAS, USA

S. Gunaseelan : R. Maskiewicz (*)

Department of Pharmaceutical Sciences( School of Pharmacy Loma Linda University 11175 Campus Street, Chan Shun Pavilion 21018 Loma Linda, California 92350, USA e-mail:


Use of coital-dependent products to prevent HIV-1 transmission has resulted in mixed success. We hypothesize that incorporation of antiviral drug candidates into a novel controlled delivery system will prolong their activity, making their use coital independent, thus increasing their chance of prophylactic success.


Tenofovir, emtricitabine, and C5A peptide HIV microbicides were mechanically incorporated into matrices comprising a series of subliming solids. Matrix sublimation rates and drug release rates were measured in three in vitro and one in vivo environments intended to model human vaginal interior. Antiviral activity studies evaluating matrix incorporated microbicides were performed using in vitro cell cultures and human ectocervical explants.


Drug release rates were identical to matrix sublimation rates, and were zero order. Differences in matrix material sublimation enthalpies determined drug release and matrix erosion rates in a thermodynamically definable manner, in vitro and in vivo. Durations of release ranging from several days to several months were readily achieved. Prolonged duration of anti HIV-1 activity was shown for matrix incorporated microbicides, using ectocervical explant and cell culture models of HIV-1 infection.


Subliming solid matrices show promise as a delivery system providing multi month intravaginal release of a wide range of HIV-1 microbicides.


Sustained Local Delivery of Structurally Diverse HIV-1 Microbicides Released from Sublimation Enthalpy Controlled Matrices

Simi Gunaseelan,1 Philippe A. Gallay,2 Michael D. Bobardt,2 Charlene S. Dezzutti,3,4 Timothy Esch,3 and Richard Maskiewiczcorresponding author1

1Department of Pharmaceutical Sciences, School of Pharmacy Loma Linda University, 11175 Campus Street, Chan Shun Pavilion 21018, Loma Linda, California 92350 USA
2Department of Immunology and Microbial Science, IMM-9 The Scripps Research Institute, 10550 North Torrey Pines Road, La Jolla, California 92037 USA
3Magee-Womens Research Institute, 204 Craft Avenue, Pittsburgh, Pennsylvania 15213 USA
4Department of Obstetrics, Gynecology and Reproductive Sciences, University of Pittsburgh, 204 Craft Avenue, Pittsburgh, Pennsylvania 15213 USA
Richard Maskiewicz, Phone: +1-909-5589473, Fax: +1-909-5580446, ude.ull@zciweiksamr.
corresponding authorCorresponding author.

//////////enthalpically controlled release, HIV-1, intravaginal delivery, prolonged antiviral effect, subliming solid matrix,


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