Objective: The objective of the present investigation was to prepare and characterize Etodolac (ETO), Polyvinyl pyrrolidone K30 (PVP K30) and Hydroxypropyl β-cyclodextrin (HPB) ternary system in order to study the effect of complexation on solubility of ETO.Methods: Physical mixtures of a drug and polymers in different weight ratios (1:1, 1:2, 1:4) were prepared to study the effect of individual polymers on solubility of ETO. Spray drying method was used to investigate the combined effect of PVP K30 and HPB on saturation solubility (SS), Dissolution efficiency (DE) and mean dissolution time (MDT) of ETO. Design of experiment (DoE) was used for preparation and optimization of ternary system. Drug polymer interactions were analyzed with Fourier transform infrared spectroscopy (FTIR), Differential scanning calorimetry (DSC), Scanning electron microscopy (SEM), Xray diffraction (XRD) and particle size analysis. Results:Results of solubility study suggested that there was significant increase in solubility of ETO with increase in the concentration of PVP K30, Polyvinyl pyrrolidone K 90 (PVP K90) and HPB (*p<0.05). This might be due to the solubilizing effect of PVP K30, PVPK90 and complex formation of ETO with HPB. Various combinations of PVP K30 and HPB prepared using DoE approach by spray drying method showed greater solubility of ETO than its physical mixtures (*p<0.05). Results of FTIR, DSC, SEM, XRD and particle size analysis revealed the interaction between ETO, PVP K30 and HPB. This suggested formation of amorphous ternary system with mean particle diameter in the range of 763±1.35 nm. Conclusion:Combine use of PVP K30 and HPB with DoE approach was an effective tool for formulating ternary system of ETO.
Background: Microsponge is a class of dosage form containing porous nature containing drug that is targeted to achieve sustained action for prolong period. Microsponge based delivery system results in drug localization on skin surface and in epidermis without moving in systemic circulation to higher extent. Methods: Present study aims to formulate the microsponge containing celecoxib by quasi emulsification solvent diffusion method. Prepared formulations were evaluated for particle size, % entrapment efficiency, production yield, surface morphology, etc. Results: Formulation F1 and E2 were considered as optimized formulation having drug loading 91±4.2 % and 91±3.1 % respectively. FTIR spectroscopy analysis indicated the chemically stable, crystalline nature of the drug in these microsponges. Small change in crystallinity of pure drug was observed in XRD study. SEM study shows good microsponge surface appearance with pores on surfaces. Average particle size of optimized microsponge formulation F1 is found to be 48 µm while E2 formulation gave microsponges with particle size of 33.7 µm. As the RPM was increased the microsponge's size was also decreased and formed microsponges were spherical and is having uniform nature. Conclusion: Finally it can be concluded that chemically stable, uniform and porous microspheres were formed using Eudragit L-100 and Ethyl cellulose.
Aim: The aim of this study was to check the effect of solubility enhancement and use of honey on anti-inflammatory and antibacterial activity of etodolac (ETO). Materials and Methods: Ternary system of ETO was prepared using polyvinylpyrrolidone K30 (PVP K30) and hydroxypropyl β-cyclodextrin (HPB) by spray drying method. Design of experiment was used for preparation and optimization of ternary system. Formulations were prepared with and without addition of honey and were evaluated for its anti-inflammatory and antibacterial activity. Antiinflammatory activity was evaluated using human red blood cell (HRBC) membrane stabilization and protein denaturation methods. Disc diffusion and well diffusion methods were used to determine antibacterial activity of prepared formulations. Results and Discussion: In HRBC membrane stabilization and protein denaturation method, the prepared ternary system formulations (without honey) achieved up to 83.3% and 83.4% inhibition; whereas, the pure sample of ETO had 58.1% and 57.8% inhibition, respectively. The antimicrobial activity was significantly affected by the type of bacteria used. In well diffusion method, run 8 showed the highest inhibitory activity of 35 ± 1.3 mm and 25 ± 1.2 mm (with honey) and 30 ± 1.1 mm and 18 ± 1.0 mm (without honey) against Bacillus subtilis and Escherichia coli, respectively. Addition of honey played a significant role in increasing the anti-inflammatory as well as antibacterial activity of all formulations. Conclusion: Use of PVP K30 and HPB in combination with honey was an effective approach to enhance the anti-inflammatory and antibacterial activity of ETO.
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