The present investigation is aimed to design a statistically optimized self-microemulsifying drug delivery system (SMEDDS) of eprosartan mesylate (EM). Preliminary screening was carried out to find a suitable combination of various excipients for the formulation. A 3(2) full factorial design was employed to determine the effect of various independent variables on dependent (response) variables. The independent variables studied in the present work were concentration of oil (X 1) and the ratio of S mix (X 2), whereas the dependent variables were emulsification time (s), globule size (nm), polydispersity index (pdi), and zeta potential (mV), and the multiple linear regression analysis (MLRA) was employed to understand the influence of independent variables on dependent variables. Furthermore, a numerical optimization technique using the desirability function was used to develop a new optimized formulation with desired values of dependent variables. The optimized SMEDDS formulation of eprosartan mesylate (EMF-O) by the above method exhibited emulsification time, 118.45 ± 1.64 s; globule size, 196.81 ± 1.29 nm; zeta potential, -9.34 ± 1.2 mV, and polydispersity index, 0.354 ± 0.02. For the in vitro dissolution study, the optimized formulation (EMF-O) and pure drug were separately entrapped in the dialysis bag, and the study indicated higher release of the drug from EMF-O. In vivo pharmacokinetic studies in Wistar rats using PK solver software revealed 2.1-fold increment in oral bioavailability of EM from EMF-O, when compared with plain suspension of pure drug.
Poor water solubility and slow dissolution rate are issues drug content and polydispersity index. The obtained for the majority of upcoming and existing biologically results showed that particle size (nm) and rate of active compounds. Simvastatin is poorly water-soluble dissolution has been improved when nanosuspension drug and its bioavailability is very low from its crystalline prepared with the higher concentration of PVPK-30 and form. The purpose of the present investigation was to Poloxamer-188 and lower concentration of SLS. The increase the solubility and dissolution rate of simvastatin by particle size and zeta potential of optimized formulation the preparation of nanosuspension by Emulsification was found to be 258.3 nm and 23.43. The rate of Solvent Diffusion Method at laboratory scale. Prepared dissolution of the optimized nanosuspension was nanosuspension was evaluated for its particle size and enhanced (90.02% in 60min), relative to plain simvastatin in vitro dissolution study and characterized by zeta (21% in 60 min), mainly due to the formation of nanosized potential, differential scanning calorimetry (DSC) and particles. These results indicate the suitability of 23 factorial X-Ray diffractometry (XRD), Motic digital microscopy, design for preparation of simvastatin loaded nanosus- entrapment efficiency, total drug content, saturated pension significantly improved in vitro dissolution rate, solubility study and in vivo study. A 23 factorial design was and thus possibly enhance fast onset of therapeutic drug employed to study the effect of independent variables, effect. In vivo study shows increase in bioavailability in amount of SLS (X1), amount of PVPK-30 (X2) and nanosuspension formulation than the plain simvastatin Poloxamer-188 (X3) and dependent variables are Total drug.
Poor water solubility and slow dissolution rate are issues polydispersity index. The obtained results showed that for the majority of upcoming and existing biologically active particlesize (nm) and rate of dissolution has been improved compounds. Simvastatin is poorly water-soluble drug and when nanosuspension prepared with the higher its bioavailability is very low from its crystalline form. The concentration of PVPK-30 with the higher concentration of purpose of the present investigation was to increase the PVP K-30 and Poloxamer-188 and lower concentration of solubility and dissolution rate of simvastatin by the SLS. The partical size and zeta potential of optimized preparation of nanosuspension by Emulsification Solvent formulation was found to be 258.3 nm and 23.43. The rate Diffusion Method at laboratory scale. Prepared nanosus- of dissolution of the optimized nanosuspension was pension was evaluated for its particle size and in vitro enhanced (90.02% in 60 min), relative to plain simvastatin dissolution study and characterized by zeta potential, (21% in 60 min), mainly due to the formation of nanosized differential scanning calorimetry (DSC) and X-Ray particles. These results indicate the suitability of 23 factorial diffractometry (XRD), motic digital microscopy, entrapment design for preparation of simvastatin loaded efficiency, total drug content, saturated solubility study and nanosuspension significantly improved in vitro dissolution in vivo study. A 23 factorial design was employed to study rate, and thus possibly enhance fast onset of therapeutic the effect of independent variables, amount of SLS (X1), drug effect. In vivo study shows increase in bioavailability in amount of PVPK-30 (X2) and Poloxamer-188 (X3) and nanosuspension formulation than the plain simvastatin dependent variables are total drug content and drug.
T he present research work involves formulation development and evaluation of nasal mucoadhesive microsphere in view to, improve bioavailability and reduce dosing regimen. Microspheres were prepared by spray drying and cross-linking method using chitosan and HPMC K4M, using 32 central composite design. Microspheres were evaluated for particle size, drug content, swelling ability, and percentage yield. Compatibility was checked by doing Fourier transform infrared spectroscopy and Differential scanning calorimetry study. The polymorphism and particle shape were studied by X-ray diffraction and scanning electron microscopy. The average particle size of spray-dried and cross-linked formulations were found in the range between 20-50 µm and 30-60 µm with percent mucoadhesion in the range of 80%-90% and 60-70%, respectively. In vitro drug release was found to be proportional to drug to polymer ratio. In vitro drug release for optimized formulation, that is, (F1), for spray-drying method and cross-linking method was found to be 88.73% and 70.93% at the end of 6 h, respectively. Release of drug from microspheres followed non-Fickian diffusion kinetics. Ex vivo studies were performed with sheep nasal mucosa for mucoadhesion, histopathological study, and drug permeation. The histopathological study indicates nonirritant nature of microsphere. The microspheres were found to be stable at accelerated storage conditions for 1 month, as per International Conference of Harmonisation guidelines.
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