A pre-formulation study of a polymeric solid dispersion of paclitaxel prepared using a quasi-emulsion solvent diffusion method to improve the oral bioavailability in rats

Piao, Hongze; Yang, Liu; Piao, Hongyu; Wang, Peixiang; Shi, Huihui; Fang, Liang; Cui, Fude

doi:10.3109/03639045.2015.1054398

Cited by 11 publications

(1 citation statement)

References 39 publications

(49 reference statements)

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“…The main reason of solubility study is to ensure the solvent drug is dissolve and suitability of solvent for development of dosage form. Solubility study of Docetaxel was done by dissolving 10 mg of drug sample in various solvents like water, ethanol, methanol, acetonitrile [5,11].…”

Section: Solubility Studymentioning

confidence: 99%

Formulation of Stable Nanoliposomes of Docetaxel: Design, Optimization, and in-vitro Characterization

Harwalkar¹,

Salunkhe

Chavan³

et al. 2020

JPRI

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Background: Liposome offers many advantages over conventional dosage forms, like increased bioavailability, possibility of releasing drug at slower and constant rate, accurate drug release. Docetaxel is approved by the FDA for the treatment of locally advanced or metastatic breast cancer, head and neck cancer, gastric cancer. Docetaxel is BCS Class 4 drug; hence efficacy can be improved with liposomal formulation. Objectives: The Present study prepared Docetaxel loaded liposomal formulation. Materials and Methods: Formulation batches were designed on the basis of solvent, lipid to cholesterol ratio, lipid to release modifier ratio, hydration temperature and various physicochemical and morphological properties of formulation were examined. The zeta potential, particle size determination, pH, stability, determination of encapsulation efficacy, morphology of formulation and in-vitro drug release were investigated. Results: The zeta potential values of FD5 and FD9 were found to be -12.6 to -12.9 mV and -10.6 to -11.9 mV respectively. The entrapment efficiency of formulations of batch FD5 and FD9 were found to be 83.20% and 85.22% respectively. By comparing both FD5 and FD9 it was found that FD9 batch is optimized than FD5 in all aspects. The formulation batch FD9 has particle size of 105 nm, zeta potential in range of -10.6 to -11.9 mV; Drug entrapment efficiency 85.22%, Assay of formulation was 99.56 % and FD9 formulation shows extended release of Drug up to 13 hours. Conclusion: The study confirmed that the Liposome formulation was successfully prepared and evaluated.

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Section: Solubility Studymentioning

confidence: 99%

Formulation of Stable Nanoliposomes of Docetaxel: Design, Optimization, and in-vitro Characterization

Harwalkar¹,

Salunkhe

Chavan³

et al. 2020

JPRI

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Improved oral bioavailability of anticancer drug tamoxifen through complexation with water soluble cyclodextrins: in vitro and in vivo evaluation

Erdoğar

Nemutlu

İskit

et al. 2019

J Incl Phenom Macrocycl Chem

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Effect of supersaturation on the oral bioavailability of paclitaxel/polymer amorphous solid dispersion

Miao

Liang

Pan

et al. 2018

Drug Deliv. and Transl. Res.

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The aim of the present investigation was to evaluate the effect of supersaturation on the oral absorption of paclitaxel (PTX) in vivo. To achieve this, a PTX amorphous solid dispersion (ASD) was prepared by the solvent cast method. Among the enteric polymers tested, hypromellose acetate succinate (HPMCAS) MF was found to be the most suitable polymer for maintaining PTX supersaturation and inhibiting crystallization in vitro. The dissolution rate and extent of the ASD was remarkably improved compared with a physical mixture (PM) of PTX, HPMCAS-MF, and Poloxamer 188 (F68), reaching an apparent drug concentration of 25-30 μg/mL and maintaining it for more than 2 h. The liquid-liquid phase separation (LLPS) concentration of PTX in the presence of HPMCAS-MF was determined to be 23 μg/mL, which was different to that of 40 μg/mL in the absence of polymer. It indicated that HPMCAS was substantially incorporated into the drug-rich phase. Also, HPMCAS could absorb to the PTX surface and provided an interfacial barrier for crystal growth, as well as retard the incorporation of PTX from solution into the growing crystal lattice. The results of X-ray diffraction, differential scanning calorimetry analysis, and transmission electron microscopy confirmed that PTX existed in the amorphous state in the solid dispersion. Compared with the PM group, the ASD prepared with HPMCAS-MF and F68 achieved a 1.78-fold increase in relative oral bioavailability, while PTX solution yielded a 1.56-fold increase, which could be explained that the solubility and the permeability of PTX were not increased simultaneously through supersaturation in vivo. Likely, it was because Cremophor inhibited P-glycoprotein in the intestine to some extent and maintained PTX at a higher concentration for a longer time.

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A pre-formulation study of a polymeric solid dispersion of paclitaxel prepared using a quasi-emulsion solvent diffusion method to improve the oral bioavailability in rats

Abstract: The PSD is a promising formulation strategy and the QESDM is a practical preparation method to implement such formulation design.

Cited by 11 publications

References 39 publications

Formulation of Stable Nanoliposomes of Docetaxel: Design, Optimization, and in-vitro Characterization

Formulation of Stable Nanoliposomes of Docetaxel: Design, Optimization, and in-vitro Characterization

Improved oral bioavailability of anticancer drug tamoxifen through complexation with water soluble cyclodextrins: in vitro and in vivo evaluation

Effect of supersaturation on the oral bioavailability of paclitaxel/polymer amorphous solid dispersion

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