Tolterodine Tartrate Proniosomal Gel Transdermal Delivery for Overactive Bladder

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.

Proniosomes derived niosomes: recent advancements in drug delivery and targeting

“…Anti-hypersensitive drug lacidipine loaded transdermal proniosomes were produced by using cremophor RH as nonionic surfactant (Soliman et al, 2016). Rajabalaya et al (2016) successfully encapsulated oxybutynin chloride in proniosomes for its transdermal delivery in overactive bladder therapy. It was obvious from the results that proniosomes provide high drug permeation and entrapment efficiency; improve therapeutic efficacy and rapid salivary secretion recovery (Rajabalaya et al, 2016).…”

“…Rajabalaya et al (2016) successfully encapsulated oxybutynin chloride in proniosomes for its transdermal delivery in overactive bladder therapy. It was obvious from the results that proniosomes provide high drug permeation and entrapment efficiency; improve therapeutic efficacy and rapid salivary secretion recovery (Rajabalaya et al, 2016). Similarly, transdermal proniosomes were designed incorporating tolterodine tartrate (TT) for the management of overactive bladder (OAB).…”

Transdermal delivery of tolterodine tartrate for overactive bladder treatment: In vitro and in vivo evaluation

“…Elshafeey et al developed controlled release of the drug into the systemic circulation with the use of TT microemulsion, which was advantageous in prevention of nocturnal enuresis with improvement in patient compliance (16). Similar studies of both oxybutynin and TT proniosomal gel were reported by our group to be suitable for transdermal route, which reduced the dry mouth eff ect compared to the oral route in our earlier studies (17,18). The drug had not been explored for transdermal delivery as a patch and this is the fi rst study that analyses the effi cacy of this formulation.…”

Formulation and Evaluation of Topical Formulation for Cutaneous Tuberculosis

“…Optimised PNG (1 g) was dissolved in 20 mL of DW and the electrode was then dipped into gel formulation and constant reading was noted. The measurements of pH of formulation were replicated three times 24 .…”

“…In vitro release studies of optimised PNG formulation was performed by Franz diffusion cell (Make: Orchid Scientifics Model: FDC03) using cellophane membrane previously soaked in phosphate buffer pH 5.5 24 for 24 h. The cellophane membrane (Make: Pal life sciences ltd. pore size=0.45µm) was mounted between the donor and receptor compartment both containing phosphate buffer pH 5.5. Weighed quantity of optimised PNG (0.3 g containing 4.4 mg of drug) was applied on donor side of the cellophane membrane.…”