Formulation andin vitro–in vivoevaluation of ketoprofen-loaded albumin microspheres for intramuscular administration

Abstract

The objective of this work was to prepare and evaluate ketoprofen-loaded albumin microspheres for intramuscular administration. Microspheres were prepared by emulsion cross-linking method using a 2(3) factorial design and the effect of different factors on entrapment efficiency was determined. Microspheres were evaluated for entrapment efficiency, percentage yield, particle size and release behaviour. Selected formulations were then tested by differential scanning calorimetry, X-ray diffraction and scanning electron microscopy. Further they were analysed for residual solvents, syringeability and stability. Microspheres were then sterilized and bioavailability studies were carried out in New Zealand white rabbits. The physical characteristics of microspheres showed that they were suitable for IM administration. The sterilization technique adopted was adequate to maintain sterility. In vivo studies showed increase in C(max), AUC, t(1/2) and MRT (p < 0.05) administered in the form of microspheres. MRT of ketoprofen was almost 3.2-times in the form of microspheres. From these results it was concluded that the developed albumin microspheres of ketoprofen is a potential delivery system for once-a-day intramuscular administration.

Thiol derivatization of Xanthan gum and its evaluation as a mucoadhesive polymer

“…The mechanism of drug release from the buccal pellets was determined by fitting the release data to several models like zero order, first order Higuchi and Korsmeyer-Peppas plots (Mathew, Devi, Prasanth, & Vinod, 2009;Higuchi, 1961).…”

Development and characterization of Eudragit based mucoadhesive buccal patches of salbutamol sulfate

“…The release rates 'k' and 'n' of each model were calculated by linear regression analysis using Microsoft Excel 2003 software. Coefficients of correlation (R 2 ) were used to evaluate the accuracy of the fit (Mathew et al, 2009;Higuchi, 1961;Korsmeyer et al, 1983;Peppas, 1985). The R 2 , 'k' and 'n' values are given in Table 4.…”

“…The samples were filtered through 0.45 lm filter and appropriately diluted with simulated saliva solution (pH 6.2) and assayed spectrophotometrically at 278 nm. The mechanism of drug release from the buccal patches was determined by finding the best fit of the release data to Higuchi and Korsmeyer-Peppas plots (Mathew et al, 2009;Higuchi, 1961).…”

Passive targeting and lung tolerability of enoxaparin microspheres for a sustained antithrombotic activity in rats

“…Spectra were then scanned in the wave number range of 4000-400 cm À1 at ambient temperature and a resolution of 4 cm À1 . All spectra were carried under vacuum to remove air humidity contribution to obtain an adequate signal to noise ratio (Mathew et al, 2009). …”