Dacarbazine nanoparticle topical delivery system for the treatment of melanoma

Hafeez, Abdul; Kazmi, Imran

doi:10.1038/s41598-017-16878-1

Cited by 63 publications

(27 citation statements)

References 51 publications

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“…In addition, the observation that AMPK is dephosphorylated in samples of tumors treated with the drug probably contributes to cancer cell death due to the inability to provide energy substrates to the growing tumor ( 41 ). Interestingly, DTIC did not reproduce these effects, nor did it exhibit a significant synergism with F10503LO1 in terms of signaling or tumor growth arrest, prevailing the action of the benzylamine derivative over the DTIC treatment ( 5 , 21 ). Complementary to these studies, the in vitro effects of F10503LO1 and F60427RS1 on melanoma cells well supported the in vivo data on tumorigenesis.…”

Section: Discussionmentioning

confidence: 99%

Benzylamine and Thenylamine Derived Drugs Induce Apoptosis and Reduce Proliferation, Migration and Metastasis Formation in Melanoma Cells

et al. 2018

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Melanomas are heterogeneous and aggressive tumors, and one of the worse in prognosis. Melanoma subtypes follow distinct pathways until terminal oncogenic transformation. Here, we have evaluated a series of molecules that exhibit potent cytotoxic effects over the murine and human melanoma cell lines B16F10 and MalMe-3M, respectively, both ex vivo and in animals carrying these melanoma cells. Ex vivo mechanistic studies on molecular targets involved in melanoma growth, migration and viability were evaluated in cultured cells treated with these drugs which exhibited potent proapoptotic and cytotoxic effects and reduced cell migration. These drugs altered the Wnt/β-catenin pathway, which is important for the oncogenic phenotype of melanoma cells. In in vivo experiments, male C57BL/6 or nude mice were injected with melanoma cells that rapidly expanded in these animals and, in some cases were able to form metastasis in lungs. Treatment with anti-tumor drugs derived from benzylamine and 2-thiophenemethylamine (F10503LO1 and related compounds) significantly attenuated tumor growth, impaired cell migration, and reduced the metastatic activity. Several protocols of administration were applied, all of them leading to significant reduction in the tumor size and enhanced animal survival. Tumor cells carrying a luciferase transgene allowed a time-dependent study on the progression of the tumor. Molecular analysis of the pathways modified by F10503LO1 and related compounds defined the main relevant targets for tumor regression: the activation of pro-apoptotic and anti-proliferative routes. These data might provide the proof-of-principle and rationale for its further clinical evaluation.

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Section: Discussionmentioning

confidence: 99%

Benzylamine and Thenylamine Derived Drugs Induce Apoptosis and Reduce Proliferation, Migration and Metastasis Formation in Melanoma Cells

et al. 2018

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“…Smaller the nanoparticle size resulted in greater surface area which leads to quick drug delivery. 26 Mean particle size consisting of all batches were found in the range of 155.5-200.4 nm. Nanoparticles comprised of batch C3 had smallest (155.5 nm) particle size.…”

Section: Particle Size Analysis and Zeta Potentialmentioning

confidence: 91%

Chitosan Loaded Ketorolac Tromethamine Nanoparticles for Improved Ocular Delivery in Eye Inflammation

Sharma¹,

Sharma²,

Sara³

et al. 2018

IJPER

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Aim: Ketorolac tromethamine (KT) is highly effective in treating post-operative eye inflammation, allergic conjunctivitis as well other ailments. It is reported that USFDA has approved a 0.45% ophthalmic solution of KT (Acuvail, Allergan, Inc) for the treatment of pain and inflammation after cataract surgery. However, the bioavailable amount of an ocular dosage form is very low due to continuous defensive mechanism in the eye. Thus the aim of present study was to improve the bioavailability of KT via sustained release using the polymer matrix (Chitosan) as a carrier. Materials and Methods: Nanoparticles of Ketorolac tromethamine were prepared by ionotropic gelation method. Design expert software was used to evaluate the effect of chitosan and tripolyphosphate (TPP) concentration on particle size and entrapment efficiency of nanoparticles. Prepared nanoparticles were physico-chemically characterized for % yield, entrapment efficiency, particle size and Zeta potential, surface morphology, in-vitro drug release, release kinetics and stability studies. In accordance with the evaluation parameters and results obtained from factorial design, an optimized batch was designed and evaluated for above mentioned parameters. Results: The optimized batch thus prepared was having Percentage yield (66.4%), Percentage Entrapment Efficiency (61.65%), Particle size (153.9 nm), Zeta Potential (-21.8) and percentage drug release (94.368±0.181 & 92.797±0.150% in PBS and STF (pH 7.4) respectively). Results of release kinetic study revealed that drug dissolution followed Zero order release kinetics model. No physicochemical changes were seen when stored at accelerated conditions. Conclusion: It was concluded that the principle adopted behind this research work will provide impetus for future researchers to carry out such formulations of wider variety of drugs rendering highly economical utility.

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“…The cumulative amount of material that was permeated into a unit region of the skin was plotted as a function of time [32][33][34].…”

Section: Skin Permeation Data Analysismentioning

confidence: 99%

Topical Drug Delivery of Gossypin From Proniosomal Gel Formulations: In Vitro Efficacy Against Human Melanoma Cells

2021

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Objective: This work aimed to establish and formulate the gossypinproniosomal gel drug delivery system. Methods: Gossypin-loaded proniosomal gels (GPG) was prepared using specific non-ionic surfactants (Spans), followed by particle size (PS), entrapment efficiency (percent EE), in vitro, ex-vivo drug release, and in vitro efficacy of Gossypin against human melanoma cells (A-375). Results: The results showed that the percentage EE for the GPG is appropriate (81.3 %–95.5 %) and they are Nano-sized (189.3–912.0 nm) and the gels diffusion provided the desired sustaining effect for GPG-F7 formulation (75.5 percent). The GPG reported cell viability of 14.9±2.3 percent compared with 16.1±1.1 percent for free Gossypin at the maximum dose of 100 μg/ml for A-375 human melanoma cells after 24 hr incubation time. No major changes were seen in the percentage EE, PS of GPG after storage for 90d, in the physical stability report. Conclusion: The results obtained suggest that the proniosomal drug delivery system can enhance the flux to the skin and achieve the ideal Gossypin sustainability effect. Consequently, the use of proniosomal gel may be advantageous with regard to the topical delivery of Gossypin for melanoma treatment management.

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Dacarbazine nanoparticle topical delivery system for the treatment of melanoma

Cited by 63 publications

References 51 publications

Benzylamine and Thenylamine Derived Drugs Induce Apoptosis and Reduce Proliferation, Migration and Metastasis Formation in Melanoma Cells

Benzylamine and Thenylamine Derived Drugs Induce Apoptosis and Reduce Proliferation, Migration and Metastasis Formation in Melanoma Cells

Chitosan Loaded Ketorolac Tromethamine Nanoparticles for Improved Ocular Delivery in Eye Inflammation

Topical Drug Delivery of Gossypin From Proniosomal Gel Formulations: In Vitro Efficacy Against Human Melanoma Cells

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