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Pharmaceutics 2016, 8(3), 27; doi:10.3390/pharmaceutics8030027

Tolterodine Tartrate Proniosomal Gel Transdermal Delivery for Overactive Bladder

1
PAPRSB Institute of Health Sciences, Universiti Brunei Darussalam, Bandar Seri Begawan BE 1410, Brunei
2
School of Pharmacy, International Medical University, Bukit Jalil, Kuala Lumpur 57000, Malaysia
3
School of Medicine, Perdana University, Jalan MAEPS Perdana, Serdang, Selangor 43400, Malaysia
*
Author to whom correspondence should be addressed.
Academic Editor: Tommasina Coviello
Received: 9 June 2016 / Revised: 25 August 2016 / Accepted: 26 August 2016 / Published: 31 August 2016
View Full-Text   |   Download PDF [13753 KB, uploaded 31 August 2016]   |  

Abstract

The goal of this study was to formulate and evaluate side effects of transdermal delivery of proniosomal gel compared to oral tolterodine tartrate (TT) for the treatment of overactive bladder (OAB). Proniosomal gels are surfactants, lipids and soy lecithin, prepared by coacervation phase separation. Formulations were analyzed for drug entrapment efficiency (EE), vesicle size, surface morphology, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, in vitro skin permeation, and in vivo effects. The EE was 44.87%–91.68% and vesicle size was 253–845 nm for Span formulations and morphology showed a loose structure. The stability and skin irritancy test were also carried out for the optimized formulations. Span formulations with cholesterol-containing formulation S1 and glyceryl distearate as well as lecithin containing S3 formulation showed higher cumulative percent of permeation such as 42% and 35%, respectively. In the in vivo salivary secretion model, S1 proniosomal gel had faster recovery, less cholinergic side effect on the salivary gland compared with that of oral TT. Histologically, bladder of rats treated with the proniosomal gel formulation S1 showed morphological improvements greater than those treated with S3. This study demonstrates the potential of proniosomal vesicles for transdermal delivery of TT to treat OAB. View Full-Text
Keywords: Proniosome; transdermal; salivary secretion; permeation; cholesterol; overactive bladder Proniosome; transdermal; salivary secretion; permeation; cholesterol; overactive bladder
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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).

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MDPI and ACS Style

Rajabalaya, R.; Leen, G.; Chellian, J.; Chakravarthi, S.; David, S.R. Tolterodine Tartrate Proniosomal Gel Transdermal Delivery for Overactive Bladder. Pharmaceutics 2016, 8, 27.

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