Anti-cancerous efficacy and pharmacokinetics of 6-mercaptopurine loaded chitosan nanoparticles

Kumar, Gaurav; Sanganal, Jagadeesh S.; Phani, A.R.; Manohara, C; Tripathi, Syamantak Mani; Raghavendra, HL; Janardhana, P.B.; Amaresha, S.; Swamy, K. B.; Prasad, R.G.S.V.

doi:10.1016/j.phrs.2015.07.025

Cited by 34 publications

(21 citation statements)

References 48 publications

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“…These approaches include liposomal delivery, micelles, microspheres and metallic and polymeric based nanoparticles (see Fig. 2) [66][67][68][69][70][71][72][73][74][75][76][77].…”

Section: Nanomedicine Approachesmentioning

confidence: 99%

“…Significant amount of cytotoxicity 48 h after nanoparticle exposure, probably caused by intracellular uptake of TG nanoparticles by pinocytosis Rajashekarajah [ 68 ] India Polymer-based drug delivery TG Chitosan In vitro (PA-1 cells) Drug release pH 4.8 > pH 7.4 of TG nanoparticles after 48 h (91.4% vs 74.0%). IC 50 values of 5.8, 12.9 and 3.9 µM for TG, curcumin and TG nanoparticles Govindappa [ 70 ] India Polymer-based drug delivery MP Chitosan In vivo (Wistar rats) This study investigated the in vivo toxicity profile of MP-NPs and MP Ahmed [ 74 ] Egypt Polymer-based drug delivery MP Chitosan In vitro (MCF-7 cells) ↑ Cytotoxicity of MP NP compared to MP Decreased cell survival of 8% (3.1 µM) and 55% (6.2 µM) for MP and MP NP Wan [ 71 ] China Polymer-based drug delivery TG Dialdehyde sodium alginate In vitro (HL-60 cells) Drug release at pH 5.0 (98.6%), no drug release at pH 7.4 Qiu [ 69 ] China Polymer-based drug delivery MP Hyaluronic In vivo (nude mice) ↑ T 1/2 , ↑ reduction tumor volume for HA-MP compared to MP ( P < 0.01) Kumar [ 72 ] India Polymer-based drug delivery MP Chitosan In vivo (Wistar rats) ↑ C max , ↑ bioavailability, ↑ T 1/2 for MP-NP compared to MP. Cmax (ng/ml) of 25.3 (at 4 h) vs 13.5 (at 2 h) for MP-NP and MP.…”

Section: Strategies For Thiopurine Drug Deliverymentioning

confidence: 99%

“…The most studied polymer for thiopurine delivery is chitosan. Thiopurine-loaded chitosan nanoparticles have been studied preclinically for thioguanine, azathioprine and mercaptopurine [ 68 , 70 , 72 , 74 , 92 ]. Chitosan nanoparticles display a pH-dependent drug release profile due to the solubility of chitosan [ 93 ].…”

Section: Strategies For Thiopurine Drug Deliverymentioning

confidence: 99%

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Advances in Thiopurine Drug Delivery: The Current State-of-the-Art

Bayoumy

Crouwel²,

Chanda

et al. 2021

Eur J Drug Metab Pharmacokinet

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Thiopurines (mercaptopurine, azathioprine and thioguanine) are well-established maintenance treatments for a wide range of diseases such as leukemia, inflammatory bowel disease (IBD), systemic lupus erythematosus (SLE) and other inflammatory and autoimmune diseases in general. Worldwide, millions of patients are treated with thiopurines. The use of thiopurines has been limited because of off-target effects such as myelotoxicity and hepatotoxicity. Therefore, seeking methods to enhance target-based thiopurine-based treatment is relevant, combined with pharmacogenetic testing. Controlled-release formulations for thiopurines have been clinically tested and have shown promising outcomes in inflammatory bowel disease. Latest developments in nano-formulations for thiopurines have shown encouraging pre-clinical results, but further research and development are needed. This review provides an overview of novel drug delivery strategies for thiopurines, reviewing modified release formulations and with a focus on nano-based formulations.

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“…These approaches include liposomal delivery, micelles, microspheres and metallic and polymeric based nanoparticles (see Fig. 2) [66][67][68][69][70][71][72][73][74][75][76][77].…”

Section: Nanomedicine Approachesmentioning

confidence: 99%

Section: Strategies For Thiopurine Drug Deliverymentioning

confidence: 99%

Section: Strategies For Thiopurine Drug Deliverymentioning

confidence: 99%

See 1 more Smart Citation

Advances in Thiopurine Drug Delivery: The Current State-of-the-Art

Bayoumy

Crouwel²,

Chanda

et al. 2021

Eur J Drug Metab Pharmacokinet

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“…Absorptions at 3400 cm -1 in [2] and 3407 cm -1 in [3] suggest υ(N-H) of pyrimidine ring of 6-mercaptopurine 9,50,58 . υ(N-H) of imidazole ring are missing due to absence of N-H bond of imidazole ring (Table 3).…”

Section: Ftir Spectramentioning

confidence: 99%

Reactions of MoO2Cl2 and MoOCl4 with 2-Mercaptopyridine, 4-Phenylimidazole-2-thiol and 6-Mercaptopurine Monohydrate

2021

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MoO2Cl2/MoOCl4 have been reacted with 4-phenylimidazole-2-thiol/6-mercaptopurine monohydrate/2-mercaptopyridine in acetonitrile solvent in unimolar/bimolar proportions at room temperature. The products thus obtained are: MoOCl3(C9H8N2S), [1]; Mo2O3Cl6(C9H7N2S)(CH3CN)2, [2]; Mo2O3Cl8(C9H7N2S)2(CH3CN)2, [3] and Mo2O4Cl4(C5H4NS-SN4C5), [4]. These products were studied by various techniques: infrared, proton NMR, liquid/gas chromatography-mass spectrometry, elemental analyses. Owing to the sensitivity of the products to air and moisture, the reactions and work ups were performed in vacuum line purged with oxygen by flushing dry nitrogen in it. Ions observed in mass spectrum are concurrent with the depicted formulae.

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“…17,19 Although 6-mercaptopurine is known for its toxicity, 20 attempts have been made to control the toxicity via polymeric-controlled drug delivery systems. 16,18 Microparticles of 6-mercaptopurine were prepared by ionic gelation and emulsification techniques using natural polymers due to their biocompatible nature. In this study, chitosan (CS), casein (CAS), and carrageenan (CRG) polymers were used along with sodium tripolyphosphate (TPP) as a crosslinker.…”

Section: Introductionmentioning

confidence: 99%

Preparation and characterization of pH-responsive ionic crosslinked microparticles of mercaptopurine to target ulcerative colitis

Hameed

Rehman

Hameed

et al. 2021

Polymers and Polymer Composites

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The objective of this study was the preparation of ionically crosslinked 6-mercaptopurine (6-MP) monohydrate microparticles through preparing polyelectrolyte complexes of drug and polymers. Polymers such as chitosan, casein, and carrageenan were used to prepare crosslinked microparticles, and sodium tripolyphosphate was used as crosslinker. Microparticles were characterized for their flow behavior, compressibility, percentage yield, micromeritic, and entrapment efficiency. Scanning electron microscopy was conducted to understand the surface morphology of the microparticles, and the result was correlated with the swelling index and percentage drug release. Mathematical modeling of drug release in order to determine the drug release kinetics was also determined to understand the mechanism involving the release of 6-mercaptopurine from the microparticles. The ionic crosslinked microparticles were in the range of 664 μm–798 μm particle size having good flow and compressibility properties with percentage yield were found to be from 77.5% to 87.5% in range. The entrapment efficiency for the formulations were found to be from 63.5% to 83.5%, with MCP-5 gave maximum entrapment efficiency of 83.5%. In vitro swelling and drug release studies were in accordance with the polymer properties following zero-order model with super-case transport II.

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Anti-cancerous efficacy and pharmacokinetics of 6-mercaptopurine loaded chitosan nanoparticles

Cited by 34 publications

References 48 publications

Advances in Thiopurine Drug Delivery: The Current State-of-the-Art

Advances in Thiopurine Drug Delivery: The Current State-of-the-Art

Reactions of MoO2Cl2 and MoOCl4 with 2-Mercaptopyridine, 4-Phenylimidazole-2-thiol and 6-Mercaptopurine Monohydrate

Preparation and characterization of pH-responsive ionic crosslinked microparticles of mercaptopurine to target ulcerative colitis

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