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In the present study, Ketoconazole loaded transfersomal formulation was developed using 3-factor, 3-level Box-Behnken design to find out the best formulation. Optimized transfersomal formulation was prepared by solvent evaporation method and evaluated in vitrofor vesicle size (126.9 ± 5.45 nm) and entrapment efficiency (82.6%). Transfersomal gel were developed by incorporation of optimized transfersomal formulation into 1% carbopol gel base and characterized by physical evaluation and rheological studies. The cumulative release of drug were shown at 72 h approximately 74% and 97% of ketoconazole from suspension and transfersomal gels respectively. The flux for transfersomal gel was found to be about 3 times that of drug suspension gel. Results of the histopathological studies of gel treated skin indicated negligible sign of toxicity and irritation. The prepared transfersomal gel showed antimicrobial activity against Candida albicans with MIC 4.57–4.6 μg/mL and better zone of inhibition as compared to reference standard. The developed gel showed promising antimicrobial activity. These overall findings suggested that transfersomal gel holds an excellent potential for ketoconazole delivery.

Topotecan being highly water-soluble drug with a property of getting converted from biologically active lactone form to biologically inactive carboxylate form, thus making it a candidate with very less bioavailability; so, our approach was to develop a stable Topotecan lactone (active) form nanoparticles (TNPs). TNPs were developed and optimized successfully with size of 130.0 ± 3.9 nm, 0.102 ± 0.009 PDI and zeta potential of −18.0 ± 2.1 mV. The percent entrapment efficiency of active lactone form of Topotecan (TOP) in optimized formulation of TNPs was 65.72 ± 1.9%, that was enhanced by approximately 15% from 65.72 ± 1.9% to 73.27 ± 2.1% by using Zn2+ions as a complexing agent between PLGA polymer and Topotecan drug. Lyophilized TNPs under DSC study showed the entrapment of TOP in amorphous or solution form, which was further confirmed by XRD studies. In vitrorelease study depicts that the drug TOP in TNPs showed initial burst release followed by sustained release for up to 72 h in PBS (pH 7.4). Ex-vivogut permeation study revealed that TNPs enhanced the permeation of TOP through the gut. Further, in vivopharmacokinetic data showed that the oral bioavailability of TOP was increased by four folds from TNPs. TNPs in comparison to TOP drug also showed a significant reduction in IC50in cell line studies on MCF-7/Adr resistant cells.

Lutein has low oral bioavailability and penetration through the skin. Therefore, the major objective is the development of ethosomal gel loaded with lutein to enhance dermal deposition of lutein. Lutein-loaded formulation (Lut-eth) was developed and optimized using QbD software. The characterization of Lut-eth formulation was performed using zeta sizing (131.3 ± 1.10 nm) and zeta potential (−21.9 mV) which was later validated by electron microscopy. The lut-eth gel was prepared and values for content uniformity, spreadability, consistency, firmness, and toughness were found to be 97.89 ± 1.05%, 7.29 ± 0.015 gcm/s, 2.495 ± 0.24 g s, 0.210 ± 0.01g, and 0.37 ± 0.01 respectively. Rheological investigation reveals viscosity was 2.56.2 mPa s (millipascal second) and shows high elasticity and stability. whereas, consistency, firmness, toughness, the force of adhesion, and work of adhesion was found to be 2.495 ± 0.24 g s, 0.210 ± 0.01g, 0.37 ± 0.01, −0.23 ± 0.05 N, and −55.61 ± 0.11 N s respectively. The lut-eth gel had a maximum plasma concentration of 9.428 ± 3.5 ng/mL in 4 h with AUC0-1279. 679 ± 9.87 ng h mL−1. The drug release study shows sustain release behavior of prepared formulation and a similar sustain release pattern was observed in and Ex-vivo release studies. Confocal laser microscopy, In-vitro,antioxidant study shows better deposition and improved antioxidant effect of formulation which was further validated by Ex-vivoantioxidant assay. Therefore, bearing in mind all these findings, it can be said that Lut-eth gel could be a novel formulation to improve lutein deposition on skin.