Objective: The main objective of the present work is the development of polymeric low-density microballoons for prolonged gastroretentive delivery and optimization of promising formulation by central composite design of response surface methodology. Methods: Mebendazole-loaded microballoons were prepared by emulsion solvent diffusion method using Eudragit S-100 and hydroxypropyl methylcellulose as release controlling polymers. All the formulations of mebendazole-loaded microballoons showed buoyancy up to 8 h. Percentage of Eudragit S-100 (X1) in total amount of polymer and solvent ratio (X2) was taken as two independent variables. The responses are evaluated to study the effect of independent variables and the optimum formulation was chosen based on numerical and graphical optimization. Results: The optimized formulation MBZ9 was composed of 100 mg of mebendazole, 75% of Eudragit S-100, and 25% of HPMC with DCM: ETH ratio of 1:1. The optimized formulation showed yield (81%), buoyancy (86.4%), entrapment efficiency (82.01%), and cumulative drug release for 12 h (79.99%). The optimized formulation was characterized by differential scanning calorimetry, and Fourier-transform infrared spectroscopy. It followed mixed order and the mechanism of drug release was diffusion as per R2=0.905 in Higuchi model. Conclusion: Microballoons of mebendazole produced with 75% Eudragit S-100, X1 (750 mg), 25% of HPMC polymer, and 1:1 DCM: ETH solvent ratio X2 (10:10 ml) optimized by response surface methodology are successful with enhanced gastroretentive effect and controlled release to elicit promising anthelminthic effect in the gastrointestinal tract.

Objective: The objective of this study is to fabricate favipiravir-loaded PLGA nanoparticulate systems that can increase the solubility along with the sustained release of favipiravir. Methods: The favipiravir-loaded Poly (D, L-lactic-co-glycolide) (PLGA) nanoparticulate systems were prepared by the nanoprecipitation method. A 3-factor, 2-level central composite face-centered design was employed to study the effect of formulation variables having a concentration of PLGA, polyvinyl alcohol (PVA) and stirring rate as critical formulation attributes and particle size, drug entrapment efficiency, and percentage cumulative drug release as critical quality attributes on prepared favipiravir nanoparticles. Drug interaction studies were performed by FTIR and DSC. Surface morphology was analysed by scanning electron microscopy (FEI Quanta 250 FEG, USA). Particle size, zeta potential, and polydispersity index were analysed by the nanoparticle analyser SZ-100 (HORIBA Scientific nanopartica, Japan). In vitro drug release studies were performed using a UV-Visible spectrophotometer at λmax 234 nm. In vitro drug release data obtained was fitted into various mathematical kinetic models. Results: The numerical optimization process predicted the level of PLGA concentration as 69.96 mg, PVA concentration as 4.99%, and stirring rate as 799 rpm for the optimised formulation. The low percentage of relative error for the optimised formulation confirms the validation of the model. The optimised formulation had a 77.65% entrapment efficiency with a particle size of 109.7 nm and the percent cumulative drug release showed 86.46% drug release over 720 min. The drug release was found to follow first-order release kinetics with anomalous non-Fickian diffusion kinetics. Conclusion: Hence, such an attempt at fabrication of favipiravir-loaded PLGA nanoparticulate systems may be useful for sustained release of drug over 720 min.

Objectives: Daclatasavir dihydrochloride (DCLD) is used to treat hepatitis C. DCLD can be used to patients with all stages of compensated liver disease including cirrhosis. The aim of the present study was to develop DCLD microspheres to improve the permeation and maximum accumulation in the liver and in vitro evaluation. Methods: DCLD microspheres were prepared with chitosan polymer using emulsion crosslinking technique. Twelve formulations were prepared, that is, F1-F12. The microspheres were evaluated for morphology, particle size, encapsulation efficiency, % yield, and permeability. FTIR studies were conducted on optimized formulation to check the drug-excipient compatibility. Results: The particle size of microspheres was in the range of 11.50±0.08 μm to 98.50±0.05 μm. Encapsulation efficiency of the formulations was observed in the range 47.8–69.2%. The ex vivo permeation studies revealed that 83.3±0.1% of drug was diffused from microspheres in 60 min, whereas from pure drug 49±0.7% of drug was diffused in 60 min. Conclusion: DCLD microspheres were shown good permeability when compared to pure drug which will improve the absorption.

Objectives: The main objective of the present work is to enhance the bioavailability of ellagic acid (EA) by increasing its dissolution there by allowing for the exploitation of its therapeutic effects. Methods: Phytosomes containing EA were prepared by anti-solvent precipitation method. The prepared phytosomes were evaluated for drug entrapment efficiency, in vitro drug release, and drug excipient interaction studies. Results: Formulation F2 containing EA and soya lecithin in the ratio (1:2) showed highest percentage of drug release as 85.40% in 60 min and 95.86% in 120 min. The drug entrapment efficiency values were satisfactory. There were no interactions between the drug and the excipients used in its preparation according to Fourier-transform infrared spectra of pure EA and EA phytosomes. Conclusion: Phytosomes of EA were successfully produced by anti-solvent precipitation method and the percentage drug entrapment efficiency was satisfactory in almost all formulations. Formulation F2 exhibited highest percent of drug release as 85.40% in 60 min and 95.86% in 120 min to possess optimum bioavailability.