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.
Highlights
Overactive bladder (OAB) syndrome was defined as “urgency, with or without urge incontinence, usually with frequency and nocturia,” by the International Continence Society [1]
The most common type of urinary incontinence among geriatric patients is urge incontinence, as bladder contraction is predominantly stimulated by parasympathetic innervation, anticholinergic agents are used for treatment and are the first-line drugs for women with overactive bladder (OAB) [3]
Among the formulations studied, the S1 gel had the most effective combination of surfactant, cholesterol, and aqueous phase
Summary
Overactive bladder (OAB) syndrome was defined as “urgency, with or without urge incontinence, usually with frequency and nocturia,” by the International Continence Society [1]. This leads to a decrease in quality of life. In Asia, the reported prevalence was even greater, 30%, and increased with age [2]. Antimuscarinics most currently used to treat OAB are oral oxybutynin, tolterodine, and trospium, which have associated side effects such as dry mouth, constipation, headache, and blurred vision, often leading to discontinuation of therapy [4,5]. Its anticholinergic side effects, especially dry mouth, have remained a common reason for therapy discontinuation [7]. It was reported that 30% of oral TT treated patients experienced
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