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Abstract Background The present research work aims to develop a Ropinirole-loaded self-Nanoemulsifying Drug Delivery system. Ropinirole has limited oral bioavailability due to substantial first-pass metabolism, which ultimately results in poor oral bioavailability and reduces plasma drug concentration and an overall reduction in therapeutic effects. Avoiding hepatic first-pass metabolism by increasing lymphatic uptake is the goal of the creation of the Ropinirole Self-NanoEmulsifying System. The solvent system for the liquid Self-NanoEmulsifying Drug Delivery System (SNEDDS) was optimized using Box-Behnken Design, where the concentration of oil(X1), surfactant (X2), and co-surfactant(X3) were taken as independent variables. The formulated liquid SNEDDS were then converted into solid SNEDDS by the adsorption method for improving patient compliance. Results The obtained mean droplet size of the formulated SNEDDS was 96.71 nm, and the rate of emulsification was 22 s. Liquid SNEDDS was converted into solid SNEDDS using Syloid 244 FP as adsorbent. Scanning Electron Microscopy (SEM) study shows well-separated particles adsorbed on Syloid 244 FP. In vitro drug release studies show better release from solid and liquid SNEDDS when compared to pure suspension. Conclusions Ropinirole-loaded SNEDDS can be a better option for reducing the extensive first-pass metabolism associated with Ropinirole.

Abstract Background Boswellic acid (BA), a phytoconstituent obtained from Boswellia serrata, suffers from several limitations after oral administration such as poor systemic absorption, high first-pass metabolism and high frequency of dose requirement, which creates a need to develop an alternative route for drug administration via novel drug delivery formulation. The present research work aims at developing ultradeformable vesicular carriers (transferosomes) for transdermal delivery of boswellic acid to effectively deliver the drug into deeper layers of the skin reaching the target site and thus improving its systemic bioavailability. Ultradeformable vesicles were prepared by thin-film hydration technique, and the formulation was optimized using 32 full factorial design where the amount of lecithin (mg) and concentration of surfactant (%) were considered as independent variables. The formulated boswellic acid-loaded vesicles were incorporated into transdermal film via solvent evaporation technique using the blend of polymers such as starch and HPMC K4M. Results The BA-loaded transferosomes were optimized based on vesicle size (nm) and drug entrapment efficiency (%EE), and the results were found to be 205.4 ± 1.215 nm and 86.39 ± 0.019%, respectively. Transmission electron microscopy (TEM) of optimized batch showed spherical shape of vesicles with identified lamellarity, surface charge of vesicles with high negative value − 15.2 mV that suggests electrostatic repulsion between vesicles, while the formulation showed good deformability index of 11.31 ± 0.032% due to use of Tween 80 as surfactant. In vitro permeation study demonstrated sustained release pattern of 96.53 ± 0.023% up to 24 h. Also, the in vitro drug diffusion study was carried out for transfersomal transdermal film which exhibited enhanced permeation and sustained retention of drug up to 94.71 ± 0.019% for 24 h. Conclusion Accordingly, the research work suggested that the transferosomes provided an efficient nanosized carriers for enhanced permeation of boswellic acid into deeper layers of skin and could successfully exhibit its therapeutic effect.

Abstract Background The polymeric spherical agglomerate of Bosentan monohydrate was prepared by crystallo-co-agglomeration technique, for enhancing the micrometric properties and solubility of the drug. The agglomerates were developed using two distinct solvents, DCM as a good solvent and bridging liquid and water as a weak solvent, respectively. Hydrophilic polymer like HPMC K100M is used as a hardening agent which gives mechanical strength to the agglomerates, and PEG6000 is used as a wetting agent. Other excipients like talc which was used as a size enhancer, and PVA was used as an emulsifier agent. The formulation was optimized by Box–Behnken design. The concentration of talc and PEG6000, as well as rotation speed, was considered as independent variables. The particle size, angle of repose, and % drug content were used as dependent variables to investigate the effect of independent variables on dependent variables. The spherical crystal agglomerates were subjected to various physicochemical evaluations. Results The results revealed that as the concentration of talc and PEG6000 increases, the sphericity and particle size of the agglomerates increase, and at a low agitation, speed agglomerates become more spherical and coarser, which is confirmed by FESEM. The characterization like FTIR confirms no interaction with excipients, while XRPD confirms the polymorphic changes, and gas chromatography (GC) confirms the concentration of residual organic solvents in PDE limits. The optimized formulation of SAs showed a good angle of repose which is 30.33 ± 0.35, and the % cumulative drug release at 20 min was 94.14 ± 0.628%. Finally, the FDTs of the optimized batch were prepared. Conclusions The comparison of the in vitro release study of pure drugs with agglomerates and fast dispersible tablets of agglomerates confirms the solubility improvement. Finally, it can be concluded that the polymorphic crystal agglomerates enhance the solubility and micrometric properties of Bosentan monohydrate.