Transdermal delivery of oxybutynin chloride proniosomal gels for the treatment of overactive bladder

Abstract

Context: Overactive bladder (OAB) is a common problem and anticholinergic drugs are first-line therapy, but they have side effects. Objective: Development of oxybutynin chloride (OC) proniosomal gels and analyses of its efficacy for OAB treatment. Materials and methods: Phase separation coacervation was used to prepare proniosomal gels using various non-ionic surfactants, lipids, soy lecithin and isopropyl alcohol. Gels were characterized with regard to entrapment efficiency (EE), vesicle size, surface morphology (using environmental scanning electron microscopy [E-SEM]), stability, attenuated total reflectance Fourier transform infrared (ATR-FTIR) spectroscopy, in vitro skin permeation, in vivo animal studies and histopathology. Results and discussion: EE was 87-92%, vesicle size was 0.38-5.0 mm, and morphology showed some loosened pores in proniosomes after hydration. ATR-FTIR spectroscopy showed no significant shifts in peaks corresponding to OC and excipients. Most formulations exhibited 450% permeation but the cholesterol-containing formulations P3 (Span 20:Span 60 [1:1]) and P4 [Tween 20:Tween 80 (1:1)] had the highest percent cumulative permeation. P3 and P4 also showed faster recovery of cholinergic effects on salivary glands than oral formulations. P3 and P4 had pronounced therapeutic effects in reduction of urinary frequency and demonstrated improvements in bladder morphology (highly regenerative surface of the transitional epithelium). Conclusion: These results suggest that OC could be incorporated into proniosomal gels for transdermal delivery in the treatment of 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.…”

“…The dermal side of the skin just touched the receptor liquid surface horizontally to allow drug permeation. The receptor compartment temperature, volume of sample collection and method of analysis were similar to the in vitro release study (17,20). The Internat ional Medical University (IMU) Research Ethics Committ ee (B0109_ Res182012) approved the procedures and animal care for the experiments undertaken in this project including pharmacological experiments.…”

“…All staining was done on at least two diff erent areas of the bladder. These were then observed under a light microscope aft er hematoxylin and eosin staining (17).…”

Development and Evaluation of Curcumin Liquid Crystal Systems for Cervical Cancer

“…LC have the ability to form an organized mesophase exhibiting both crystalline solid and liquid properties [12]. The LC system has unique microstructure and physicochemical properties, whereby it can potentially solubilize oil and water-soluble compounds and thus can be used as a drug carrier system for both hydrophilic and hydrophobic drugs [13,14]. The incorporation of drugs in liquid crystals irrespective of their relative affinity towards hydrophilic or hydrophobic solvents is exploited in the field of biological sensing and drug delivery for various drug categories and formulations, i.e., analgesics, anti-cancer agents, drugs for liver diseases, anti-asthmatic drugs, nanoparticles formulations, and others [15].…”

Novel non-ionic surfactant proniosomes for transdermal delivery of lacidipine: optimization using 23factorial design andin vivoevaluation in rabbits

“…Proniosomes were prepared by a coacervation phase separation method (Gadekar et al, 2013;Ramkanth et al, 2014;Rajabalaya et al, 2015). Precisely weighed amounts of surfactant, soya lecithin, cholesterol, and drug were taken in a clean and dry wide mouthed glass vial of 5.0 ml capacity and absolute ethanol (0.25 ml) was added to it.…”