Development and evaluation of exemestane-loaded lyotropic liquid crystalline gel formulations

Abstract

Introduction: The use of liquid crystalline (LC) gel formulations for drug delivery has considerably improved the current delivery methods in terms of bioavailability and efficacy. The purpose of this study was to develop and evaluate LC gel formulations to deliver the anti-cancer drug exemestane through transdermal route. Methods: Two LC gel formulations were prepared by phase separation coacervation method using glyceryl monooleate (GMO), Tween 80 and Pluronic® F127 (F127). The formulations were characterized with regard to encapsulation efficiency (EE), vesicle size, Fourier transform infrared (FTIR) spectroscopy, surface morphology (using light and fluorescence microscopy), in vitro release, ex vivo permeation, in vitro effectiveness test on MDA-MB231 cancer cell lines and histopathological analysis. Results: Results exhibited that the EE was 85%-92%, vesicle size was 119.9-466.2 nm while morphology showed spherical vesicles after hydration. An FTIR result also revealed that there was no significant shift in peaks corresponding to Exemestane and excipients. LC formulations release the drug from cellulose acetate and Strat-MTM membrane from 15%-88.95%, whereas ex vivo permeation ranges from 37.09-63%. The in vitro effectiveness study indicated that even at low exemestane concentrations (12.5 and 25 μg/mL) the formulations were able to induce cancer cell death, regardless of the surfactant used. Histopathological analysis thinning of the epidermis as the formulations penetrate into the intercellular regions of squamous cells. Conclusion: The results conjectured that exemestane could be incorporated into LC gels for the transdermal delivery system and further preclinical studies such as pharmacokinetic and pharmacodynamic studies will be carried out with suitable animal models.

The efficacy ofOriganum majoranananocubosomal systems in ameliorating submandibular salivary gland alterations in streptozotocin-induced diabetic rats

“…A similar finding was observed by Musa et al. ( 2017 ). This could be explained in terms of the high molecular weight of PF127 compared to T80 that occupies a larger area and subsequently results in a higher NC size.…”

“…This could be explained in terms of the high molecular weight of PF127 compared to T80 that occupies a larger area and subsequently results in a higher NC size. Moreover, the small PS of the formulated T80-based cubosomes can be additionally explained by their high ZP values that generate a high repulsive force, preventing particle–particle aggregation, which may be encountered with PF127-based NC dispersion (Musa et al., 2017 ).…”

Dynamic Light Scattering and Zeta Potential Studies of Ceria Nanoparticles

“…Similar adsorption behavior occurs during addition of excess volume of DEA from 0.5 to 2 ml in both aqueous concentrations. These adsorption-desorption studies could be utilized for a wide range of applications such as heavy metal removal from waste water [9]. The plots of the surface charge study (zeta potential) is presented in fig.…”

“…Cerium (IV) oxide nanoparticles, NPs (nanoceria) with chemical formula, CeO 2 is among the nanomaterials that have been largely utilized in different applications such as heavy metals removal from aqueous solution, and biomedical application [9], [10]. Nanoceria could be prepared through a number of techniques including precipitation, sol-gel and solvothermal methods.…”

Smart phase transformation system based on lyotropic liquid crystalline@hard capsules for sustained release of hydrophilic and hydrophobic drugs

“…The special structures provide incorporation of drugs with different solubility, including hydrophilic, hydrophobic and amphiphilic molecules (Conn & Drummond, 2013;Rajabalaya et al, 2017) and also tunable release rate (Rizwan & Boyd, 2015;Abd-Allah et al, 2016;Huang & Gui, 2018). LLC exhibits perfect performance on mucosal (Huang et al, 2017), transdermal (Peng et al, 2015;Musa et al, 2017), periodontal (Mei et al, 2017a;Zheng et al, 2018), subcutaneous (Mei et al, 2017b) and other parenteral drug delivery (Wan et al, 2015;Qin et al, 2016), due to its high drug-loading capacity, appropriate viscoelasticity and good biocompatibility (Abd-Allah et al, 2016;Kulkarni & Thareja, 2016).…”