Abstract
Objective: The present investigation was aimed to optimize the formula of paclitaxel-loaded liposomes (PTL) by using the application of response surface methodology (RSM).Methods: Paclitaxel-loaded liposome (PTL) was optimized by response surface methodology based on two parameters, namely, percent entrapment efficiency (% EE) and percent in vitro drug release at 12 h (% DR). The liposome formula was prepared using 32 factorial design, and the selected independent variables were, phospholipid (phospholipon 90G) and cholesterol (CH) concentrations. Nine formulas of paclitaxel-loaded liposome were prepared by thin film hydration technique (THF). The entrapment efficiency, in vitro release studies and drug content, were evaluated using on UV-visible spectrophotometer at λmax-230 nm. The developed PTL formulation vesicle morphology, particle size, polydispersity index (PDI) and zeta potential (ζ) were evaluated by Motic digital microscope and Malvern zetasizer respectively.Results: Using response surface methodology the estimated coefficient values obtained for independent variables in the regression equations, exhibited that the phospholipid (PL90G) and cholesterol (CH) molar concentration was observed to be highly influencing variables in optimizing % EE (86.67±0.67) and % DR (63.49±1.21). In the prediction of % EE and % DR values, the percent relative errors (PRE) was found to be low (–0.290%) and (0.058%) respectively. This suggests that design-developed model was found to be suitable for PTL formulations and thus, validate the model.Conclusion: Experimental results show that the observed responses were in close agreement with the predicted values and this demonstrates the reliability of the RSM in an optimization of % EE and % DR in paclitaxel liposomal (PTL) formulations.
Highlights
IntroductionPaclitaxel (PT) is a chemical compound isolated from the bark of Taxus brevifolia (northwest Pacific Yew Tree), empirical formula (C47H51NO14) and on the basis of characterization named it as Taxol [1]
Paclitaxel (PT) is a chemical compound isolated from the bark of Taxus brevifolia, empirical formula (C47H51NO14) and on the basis of characterization named it as Taxol [1]
To evaluate the quantitative effects of factors (X1 and X2) and their levels low (-1), middle (0), and high (+1) on the preferred responses, the experimental values of the flux were analyzed by Design Expert® DX 10.0.7.0 license version software and mathematical models obtained for each response [25,26, 30,31]
Summary
Paclitaxel (PT) is a chemical compound isolated from the bark of Taxus brevifolia (northwest Pacific Yew Tree), empirical formula (C47H51NO14) and on the basis of characterization named it as Taxol [1]. The diluted formulation showed the precipitation of PT from solution due to low solubility [8] These attempted techniques, with persistent low solubility problem, has been overcome by creating novel formulation with the aim of improving aqueous solubility, permeability, and bioavailability of PT. It includes novel oral formulation [9], novel PT self-emulsifying drug delivery system (SEDDS) [10], novel ligands based PT targeting formulation [11], micellar formulation [12], liposomal formulation [13], bioconjugates [14], dendrimers [15] and nanocarrier systems [16]. In all these formulation techniques the problem associated with PT was shown to be improved significantly
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