Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity

Valicherla, Guru R.; Dave, Kandarp M.; Syed, Anees A.; Riyazuddin, Mohammed; Gupta, Anand P.; Singh, Atul Kumar; Wahajuddin,; Mitra, Kalyan; Datta, Dipak; Gayen, Jiaur R.

doi:10.1038/srep26895

Cited by 90 publications

(52 citation statements)

References 26 publications

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“…Supplementary Table 1 Although several literature reports (Patil et al, 2015;Singh et al, 2016;Valicherla et al, 2016) have documented the use of lipidic systems for BCS Class II and IV bioactives like Mgf, yet the current studies endeavoured at developing the PLCs-loaded with NLCs systematically for enhance the oral bioavailability.…”

Section: Defining the Qtppmentioning

confidence: 99%

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

Khurana

Bansal

Beg

et al. 2017

International Journal of Pharmaceutics

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Mangiferin (Mgf), largely expressed out from the leaves and stem bark of Mango, is a potent antioxidant. However, its in vivo activity gets tremendously reduced owing to poor aqueous solubility and inconsistent gastrointestinal absorption, high hepatic first-pass metabolism and high P-gp efflux. The current research work, therefore, was undertaken to overcome the biopharmaceutical hiccups by developing the Mgfphospholipid complex (PLCs) loaded in nanostructured lipidic carriers (NLCs). The PLCs and NLCs were prepared using refluxing, solvent evaporation and hot emulsification technique, respectively with various molar ratios of Mgf and Phospholipon 90 G, i.e., 1:1; 1:2; and 1:3. The complex was evaluated for various physicochemical parameters like drug content (96.57%), aqueous solubility (25-fold improved) and oil-water partition coefficient (10-fold enhanced). Diverse studies on the prepared complex using FTIR, DSC, PXRD and SEM studies ratified the formation of PLCs at 1:1 ratio. The PLCs were further incorporated onto NLCs, which were systematically optimized employing a face centered cubic design (FCCD), while evaluating for particle size, zeta potential, encapsulation efficiency and in vitro drug release as the CQAs. Caco-2 cell line indicated insignificant cytotoxicity, and P-gp efflux, bi-directional permeability model and in situ perfusion studies specified enhanced intestinal permeation parameters. In vivo pharmacokinetic studies revealed notable increase in the values of Cmax (4.7-fold) and AUC (2.1-fold), respectively, from PLCs-loaded NLCs vis-à-vis Mgf solution. In a nutshell, the promising results observed from the present research work signified boosted biopharmaceutical potential of the optimized PLCs-loaded NLCs for potentially augmenting the therapeutic efficacy of Mgf.

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Section: Defining the Qtppmentioning

confidence: 99%

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

Khurana

Bansal

Beg

et al. 2017

International Journal of Pharmaceutics

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“…The commercial formulation, Taxotere Ò , employs the surfactant polysorbate 80 and ethanol to improve the solubility, although causing several side effects. [3][4][5] The mechanism of action of DTX is related to the cytotoxic activity, consequence of b-tubulin binding, which causes inhibition of cell proliferation and mitotic progression due to inhibition of microtubule dynamics. [6] DTX was approved by the Food and Drug Administration (FDA) in 1996 for the treatment of anthracycline-refractory metastatic breast cancer.…”

Section: Introductionmentioning

confidence: 99%

A Critical Review of Properties and Analytical Methods for the Determination of Docetaxel in Biological and Pharmaceutical Matrices

Hanck-Silva

Fernandes

Trevizan

et al. 2018

Critical Reviews in Analytical Chemistry

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Docetaxel (DTX) is an antineoplastic agent of the second generation of the taxoid family. It is a semi-synthetic drug prepared from a precursor extracted of the plant Taxus baccata. The commercial formulation of DTX, Taxotere®, employs the surfactant polysorbate 80, due to the low water solubility of the drug, causing several side effects. Therefore, there is a need to develop delivery systems to reduce the side effects of DTX. In addition, this drug has been qualitative and quantitatively analyzed in pharmaceutical formulations and biological samples. Thus, several techniques and analytical methods have been reported with the aim of optimizing the analytical signal, increasing sensitivity, selectivity and reducing the effects of interference. Herein, we highlight immunoassay, capillary electrophoresis and chromatographic methods. This review presents a summary of physicochemical and pharmacokinetics properties, mechanisms of action, drug delivery systems and analytical methods used in quantification of DTX in diverse matrices such as blood, plasma, oral fluid, urine, carcinoma cells, pharmaceutical formulations and delivery systems.

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“…60 Chylomicrons are triglyceride-rich lipoprotein emulsions, dietary lipids absorbed through the intestine membrane in to blood circulation are packed into chylomicrons. 61,62 Lipase is a lipoprotein enzyme which can hydrolyze the core triglycerides of the chylomicron in blood circulation. On the surface of the chylomicron, many different apolipoprotiens are anchored by their receptors receptors these modified chylomicrons are taken up by liver parenchymal cells.…”

Section: Chylomicron Emulsionmentioning

confidence: 99%

Drug targeting strategies for liver cancer and other liver diseases

Shilpi¹

2018

MOJDDT

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Treatment of liver cancer and other diseases are a challenging task for the current researchers in the pharmaceutical field. There are some physiological barriers like RES uptake, opsonization and first-pass metabolism of therapeutics present that make drug therapy more complex. Generally, conventional cancer therapy approaches give low response rate or remain un-success due to multi drug resistance (MDR), high clearance rate, severe adverse effect due to unwanted drug distribution and inadequate concentration reached in cancer cells. Therefore it is a need to develop novel strategies which will target drug molecule specific to affected liver cells. In the current era of research and development, various approaches have been utilized to improve the drug delivery and drug targeting. The new targeting approaches are based on the use of targeting ligands which can conjugate with nanocarrier or with drug molecules. These conjugates systems are accumulate passively or actively. This review focus on some liver cancer cells specific targeting ligands such as manos6 phosphate, asialoglycoprotein, galactoside, lactobionic acid, PDGF, antibodies, aptamers, avimers which have been utilized to target cancer cell after conjugation with the therapeutic system. This review also describes the novel targeting approaches including latest targeting molecules and targeted drug delivery system used for the treatment of liver cancer.

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Formulation optimization of Docetaxel loaded self-emulsifying drug delivery system to enhance bioavailability and anti-tumor activity

Cited by 90 publications

References 26 publications

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

Enhancing biopharmaceutical attributes of phospholipid complex-loaded nanostructured lipidic carriers of mangiferin: Systematic development, characterization and evaluation

A Critical Review of Properties and Analytical Methods for the Determination of Docetaxel in Biological and Pharmaceutical Matrices

Drug targeting strategies for liver cancer and other liver diseases

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