Potential of erlotinib cyclodextrin nanosponge complex to enhance solubility, dissolution rate,  in vitro  cytotoxicity and oral bioavailability

Dora, Chander Parkash; Trotta, Francesco; Kushwah, Varun; Devasari, Naresh; Singh, Charan; Suresh, Sarasija; Jain, Sanyog

doi:10.1016/j.carbpol.2015.10.080

Cited by 117 publications

(52 citation statements)

References 38 publications

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“…MTT assay was employed to determine the cell cytotoxicity of samples in MCF-7 and MDA-MB-231 cell lines, following our previously reported protocol (Dora et al, 2016). Briefly, both the cell lines were seeded to 96-well tissue culture plates and kept overnight.…”

Section: In Vitro Cytotoxicity Assaymentioning

confidence: 99%

Implication of linker length on cell cytotoxicity, pharmacokinetic and toxicity profile of gemcitabine-docetaxel combinatorial dual drug conjugate

Kushwah

Katiyar

Agrawal

et al. 2018

International Journal of Pharmaceutics

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The present study investigates effect of linkers [zero length (without linker), short length linker (glycine and lysine) and long length linker (PEG1000, PEG2000 and PEG3500)] on pharmacokinetics and toxicity of docetaxel (DTX) and gemcitabine (GEM) bio-conjugates. Conjugates were synthesized via carbodiimide chemistry and characterized by H NMR and FTIR. Conjugation of DTX and GEM via linkers showed diverse physiochemical and plasma stability profile. Cellular uptake mechanism in MCF-7 and MDA-MB-231 cell lines revealed clathrin mediated internalization of bio-conjugates developed by using long length linkers, leading to higher cytotoxicity compared with free drug congeners. DTX-PEG3500-GEM and DTX-PEG2000-GEM demonstrated 4.21 and 3.81-fold higher AUC of GEM in comparison with GEM alone. DTX-PEG2000-GEM and DTX-PEG3500-GEM exhibited reduced hepato-, nephro- and haemolytic toxicity as evident via histopathology, biochemical markers and SEM analysis of RBCs. Conclusively, PEG2000 and PEG3500 significantly improved pharmacokinetics without any sign of toxicity and hence can be explored further for the development of dual-drug conjugates for better therapeutic efficacy.

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Section: In Vitro Cytotoxicity Assaymentioning

confidence: 99%

Implication of linker length on cell cytotoxicity, pharmacokinetic and toxicity profile of gemcitabine-docetaxel combinatorial dual drug conjugate

Kushwah

Katiyar

Agrawal

et al. 2018

International Journal of Pharmaceutics

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“…Due to this characteristics nature, CDs have attained a great interest as a solubilising candidate and has overcome the biopharmaceutical deficiencies of various drugs in the recent years. 14,[17][18][19] CDs are widely soluble in some polar, aprotic solvents, but insoluble in most organic solvents. 20 Although, CDs exhibit higher solubility in some of the organic solvents than in water, inclusion complexes do not take place in non-aqueous solvents because of the increased affinity of guest molecule for the solvent compared to its affinity for water.…”

Section: Structure Of Cdsmentioning

confidence: 99%

Cyclodextrin: A Promising Candidate in Enhancing Oral Bioavailability of poorly Water Soluble Drugs

Maheriya¹

2017

MOJBB

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Most of the drugs administered through oral route have poor aqueous solubility and dissolution rate. Cyclodextrin and its derivates represent as pharmaceutical adjuvants to overcome this challenges and helps in development of stable formulation with enhanced bioavailability. Cyclodextrins are unique structure with versatile physicochemical properties which aids the pharmaceutical scientists to overcome drug delivery challenges for poorly aqueous soluble drugs. Cyclodextrin and its derivates are widely useful as solubilizers, assisting in preparation of various dosage forms such as liquid oral, solid, and parenteral preparations. Cyclodextrins interacts with appropriately sized guest molecules to form inclusion complex and enhance the aqueous solubility, physical chemical stability, and bioavailability of drugs. Through the various reported literatures, the review highlights the concept of cyclodextrin and its derivatives in enhancing solubility and bioavailability of poorly aqueous soluble drugs.

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“…The in vitro therapeutic efficacy of DTX loaded AA-GEM-BSA NPs was further assessed as a capability to induce apoptosis in MCF-7 and MDA-MB-231 cells, via standard phosphatidyl serine externalization assay based on Annexin-V binding. [21] Briefly, MCF-7 and MDA-MB-231 cells were seeded at a density of 5x10 4 cells per well in the 6-well tissue culture plate (Costars, Corning Inc., NY, USA) and kept to attach overnight at 37 ºC and 5% CO 2 . The media was then aspirated and cells were treated with media containing samples, equivalent to 10 µg/ml of DTX.…”

Section: Annexin-v Apoptosis Assaymentioning

confidence: 99%

Co-delivery of docetaxel and gemcitabine by anacardic acid modified self-assembled albumin nanoparticles for effective breast cancer management

Kushwah¹,

Katiyar

Dora

et al. 2018

Acta Biomaterialia

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The present report is the original state of art technology to selectively target dual drug (DTX and GEM) loaded BSA NPs via exploring tumor targeting potential of AA, having high affinity towards VEGF receptors (angiogenesis marker) overexpressed in tumor. The AA and GEM bio-conjugated BSA was synthesized and further used to develop DTX loaded nanoparticles (AA-GEM-BSA NPs). The optimized NPs were further evaluated via extensive in vitro and in vivo studies, demonstrating ameliorated cellular uptake, pharmacokinetic and toxicity profile of drugs. Conclusively, DTX loaded AA-GEM-BSA NPs, holds promising potential in increasing the therapeutic efficiency of drugs and overcoming solvent and drug mediated side effects and can be explored further as a scalable platform technology for difficult to deliver drugs.

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Potential of erlotinib cyclodextrin nanosponge complex to enhance solubility, dissolution rate, in vitro cytotoxicity and oral bioavailability

Cited by 117 publications

References 38 publications

Implication of linker length on cell cytotoxicity, pharmacokinetic and toxicity profile of gemcitabine-docetaxel combinatorial dual drug conjugate

Implication of linker length on cell cytotoxicity, pharmacokinetic and toxicity profile of gemcitabine-docetaxel combinatorial dual drug conjugate

Cyclodextrin: A Promising Candidate in Enhancing Oral Bioavailability of poorly Water Soluble Drugs

Co-delivery of docetaxel and gemcitabine by anacardic acid modified self-assembled albumin nanoparticles for effective breast cancer management

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