FORMULATION AND EVALUATION OF GEL LOADED WITH MICROSPHERES OF APREMILAST FOR TRANSDERMAL DELIVERY SYSTEM

Objective: The main objective of the present research work was to formulate and evaluate gel loaded with microspheres of apremilast to increase bioavailability and to reduce the dosing frequency and to improve patient compliance. Methods: Gel loaded with microspheres of apremilast was prepared by solvent evaporation method by taking different ratios of polymers. Ethyl cellulose as a polymer, dichloromethane solvent is used as drug solubility, polyvinyl alcohol as a surfactant, and sodium alginate is used as gelling agent. Prepared gel loaded with microspheres was evaluated for drug interactions by Fourier transform infrared (FTIR), differential scanning calorimetry studies, and surface morphology by scanning electron microscopy (SEM), to select effective one among all formulations. The prepared formulations (F1–F6) were evaluated for pre-formulation studies, spreadability, viscosity, pH measurement, gel strength, homogeneity, drug content, in vitro diffusion studies, drug kinetics, and finally for stability studies. Results: Differential scanning calorimeter studies confirmed that there is no drug interaction between drug and excipients. FTIR spectroscopy studies confirmed that there is compatibility between drug and excipients. Regular and spherical shape particles with smooth surface were observed in the SEM photographs. The optimized gel loaded with microspheres of F4 formulation (drug: polymer in 1:4 ratio) is more effective compared to all formulations. The prepared gel showed acceptable physical properties such as spreadability (5.86±0.54 g.cm/s), viscosity (568 cps), pH (6.33±0.55), gel strength (38 s) and drug content (90.00±0.71%). In vitro diffusion studies have shown 80.1±1.92% drug release in 10 h. Drug kinetics follows zero order kinetics and n value was found to be 0.721. Stability studies were done for 3 months. Conclusion: All the results show that the gel loaded with microspheres of apremilast can be effectively used for the treatment of psoriasis and psoriatic arthritis

Preparation and Evaluation of Tapentadol Hydrochloride Solid Lipid Nanoparticles

Tapentadol Hydrochloride is a centrally acting opioid analgesic used for the treatment of musculoskeletal pain. The aim of the present study is to release the drug at a controlled rate by formulating solid lipid nanoparticles using Hot Homogenization method. In the present study SLN’s are prepared by using Glycerol Monostearate and Stearic acid as lipids and Poloxamer-188 as stabilizer in different ratios in order to get the optimized formulation. The solid lipids and drug were evaluated for drug interactions by using FTIR, DSC, and surface morphology by SEM in order to select the effective formulation. The prepared formulations (F1-F12) were evaluated for Particle size, Zeta potential, %Entrapment efficiency, in vitro drug release studies and stability studies. The FTIR spectra revealed that there is no significant interaction between the drug and lipids. SEM images revealed that the particles are spherical in shape with smooth surface. The particle size was found as 101.9 nm, Zeta potential was found as -18.1mV, % Entrapment Efficiency (%EE) was found as 88.7±0.36 and the % drug release was found as 97.8±0.60 in 10 hours following first order release kinetics and Higuchi model. The Tapentadol Hcl loaded SLN’s of F3 formulation shows more effective when compared to all the other formulations. All the results shows that the Tapentadol Hcl SLN’s can be effectively used for treating severe pain by controlling the rate of release at the targeted site. Keywords: Tapentadol Hydrochloride, Glycerol Monostearate, Stearic acid, Poloxamer-188, Hot Homogenoisation method

PREPARATION AND IN VITRO EVALUATION OF METOPROLOL-LOADED BOVINE SERUM ALBUMIN NANOPARTICLES

Objective: The aim of the present research was to prepare metoprolol-loaded nanospheres. Metoprolol-loaded bovine albumin nanospheres were prepared by nanoprecipitation method. Metoprolol is beta-1-adrenergic receptor inhibitor specific to cardiac cells, thus producing negative chronotropic and ionotropic effect. Methods: Metoprolol nanospheres were prepared by nanoprecipitation method, using bovine serum albumin as polymer. The prepared nanospheres are evaluated for particle size evaluation, drug entrapment efficiency, and zeta potential. Drug-excipient compatibility was determined using Fourier-transform infrared spectroscopy. In vitro release and solubility of the drug from nanoparticles were determined. Results: The particle size of prepared metoprolol nanospheres was found to be always less than 200 nm. Maximum particle size was found to be 196±2.03 nm of batch 4 nanoparticles. Entrapment efficiency of prepared nanospheres was above 80% and maximum percentage entrapment efficiency was found to be 80.4±0.51%. It was found that the percentage entrapment efficiency and drug release were extended with increase in polymer concentration. Zeta potential of the optimized formulation was found to be −20.4 mV. In vitro drug release studies have shown the prolonged release of 94.5±0.54 up to 10 h. Drug release rate is extended with an increase in polymer concentration. Conclusion: Results have concluded that the albumin nanospheres loaded with metoprolol have reduced the blood pressure within 24 h and the prepared nanospheres are effective compared to other formulations and drug delivery