Paclitaxel and its formulations

Singla, Anil Kumar; Garg, Alka B.; Aggarwal, Deepika

doi:10.1016/s0378-5173(01)00986-3

Cited by 953 publications

(646 citation statements)

References 63 publications

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“…Reports of paclitaxel IC 50 value in various cell lines range from 0.7 to 5 nM [18][19][20]. The clinically recommended concentration of paclitaxel is 0.35-14 mM [21], which are several folds higher than the IC 50 value. Thus, we selected 5 nM as representative IC 50 concentration and 600 nM (which is several folds higher than the IC 50 value) as the representative clinical concentration.…”

Section: Monolayer Experimentsmentioning

confidence: 99%

Comparison of paclitaxel penetration in normal and cancerous cervical model monolayer membranes

Preetha

Huilgol

Banerjee

2006

Colloids and Surfaces B: Biointerfaces

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Section: Monolayer Experimentsmentioning

confidence: 99%

Comparison of paclitaxel penetration in normal and cancerous cervical model monolayer membranes

Preetha

Huilgol

Banerjee

2006

Colloids and Surfaces B: Biointerfaces

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“…Poor drug solubility is also a great challenge in drug development. The commonly used anti-cancer agent paclitaxel is a potent inhibitor of mitosis but is poorly soluble in water (aqueous solubility is around 0.6 mM) 2 . Paclitaxel is therefore administered in conjunction with the stabilizing agent Kolliphor EL (formally known as Cremophor EL) to ensure that therapeutically sufficient doses are delivered to the patient.…”

Section: Introductionmentioning

confidence: 99%

Polymersome-Mediated Delivery of Combination Anticancer Therapy to Head and Neck Cancer Cells: 2D and 3D in Vitro Evaluation

et al. 2014

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Polymersomes have the potential to encapsulate and deliver chemotherapeutic drugs into tumour cells, reducing off-target toxicity that often compromises anti-cancer treatment. Here we assess the ability of the pH-sensitive poly 2-(methacryloyloxy)ethyl phosphorylcholine (PMPC)-poly 2-(diisopropylamino)ethyl methacrylate (PDPA) polymersomes to encapsulate chemotherapeutic agents for effective combinational anti-cancer therapy. Polymersome uptake and ability to deliver encapsulated drugs into healthy normal oral cells and oral head and neck squamous cell carcinoma (HNSCC) cells was measured in two and three-dimensional culture systems. PMPC-PDPA polymersomes were more rapidly internalised by HNSCC cells compared to normal oral cells. Polymersome cellular up-take was found to be mediated by class B scavenger receptors.We also observed that these receptors are more highly expressed by cancer cells compared to normal oral cells, enabling polymersome-mediated targeting. Doxorubicin and paclitaxel were encapsulated into pH-sensitive PMPC-PDPA polymersomes with high efficiencies either in isolation or as a dual-load for both singular and combinational delivery. In monolayer culture, only a short exposure to drug-loaded polymersomes was required to elicit a strong cytotoxic effect. When delivered to three-dimensional tumour models, PMPC-PDPA polymersomes were able to penetrate deep into the centre of the spheroid resulting in extensive cell damage when loaded with both singular and dual-loaded chemotherapeutics. PMPC-PDPA polymersomes offer a novel system for the effective delivery of chemotherapeutics for the treatment of HNSCC.Moreover, the preferential internalisation of PMPC polymersomes by exploiting elevated scavenger receptor expression on cancer cells opens up the opportunity to target polymersomes to tumours.3

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“…The drug interacts with tubulin dimers in the G2 phase of the mitotic cell cycle to promote microtubule polymerization; the resulting formation of highly stable microtubules prevents cell division and accounts for the cytotoxic properties of Ptx (Singh et al, 2008). Ptx has excellent therapeutic efficacy against a variety of solid tumors, including breast cancer, ovarian carcinoma, lung cancer, head-and-neck carcinoma, and acute leukemia (de Bree et al, 2006;Singla et al, 2002;Fjällskog et al, 1993). However, Ptx is a hydrophobic molecule that is poorly soluble in water.…”

Section: Introductionmentioning

confidence: 99%

In vivo efficacy of paclitaxel-loaded injectable in situ-forming gel against subcutaneous tumor growth

Lee

Kim

Kang

et al. 2010

International Journal of Pharmaceutics

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Paclitaxel and its formulations

Cited by 953 publications

References 63 publications

Comparison of paclitaxel penetration in normal and cancerous cervical model monolayer membranes

Comparison of paclitaxel penetration in normal and cancerous cervical model monolayer membranes

Polymersome-Mediated Delivery of Combination Anticancer Therapy to Head and Neck Cancer Cells: 2D and 3D in Vitro Evaluation

In vivo efficacy of paclitaxel-loaded injectable in situ-forming gel against subcutaneous tumor growth

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