In-vivo evaluation of clindamycin release from glyceryl monooleate-alginate microspheres by NIR spectroscopy

Citation:
Kassem, M. A., A. M. I. R. I. B. R. A. H. I. M. MOHAMED, S. U. Z. A. N. AMIN, and O. A. A. Ahmed, "In-vivo evaluation of clindamycin release from glyceryl monooleate-alginate microspheres by NIR spectroscopy", International Journal of Pharmaceutics, vol. 494 , pp. 127–135, 2015.

Abstract:

The purpose of this study was to use near-infrared (NIR) transmission spectroscopic technique to determine clindamycin plasma concentration after oral administration of clindamycin loaded GMO-alginate microspheres using rabbits as animal models. Lyophilized clindamycin–plasma standard samples at a concentration range of 0.001–10 mg/ml were prepared and analyzed by NIR and HPLC as a reference method. NIR calibration model was developed with partial least square (PLS) regression analysis. Then, a single dose in-vivo evaluation was carried out and clindamycin–plasma concentration was estimated by NIR. Over 24 h time period, the pharmacokinetic parameters of clindamycin were calculated for the clindamycin loaded GMO-alginate microspheres (F3) and alginate microspheres (F2), and compared with the plain drug (F1). PLS calibration model with 7-principal components (PC), and 8000–9200 cm _1 spectral range shows a good correlation between HPLC and NIR values with root mean square error of cross validation (RMSECV), root mean square error of prediction (RMSEP), and calibration coefficient (R2) values of 0.245, 1.164, and 0.9753, respectively, which suggests that NIR transmission technique can be used for drug-plasma analysis without any extraction procedure. F3 microspheres exhibited controlled and prolonged absorption Tmax of 4.0 vs. 1.0 and 0.5 h; Cmax of 2.37 _ 0.3 vs. 3.81 _0.8 and 5.43 _ 0.7 mg/ml for F2 and F1, respectively. These results suggest that the combination of GMO and alginate (1:4 w/w) could be successfully employed for once daily clindamycin microspheres formulation which confirmed by low Cmax and high Tmax values.