Complexation of carbendazim with hydroxypropyl-β-cyclodextrin to improve solubility and fungicidal activity

Ge, Xin; Huang, Zheng; Tian, Shilong; Huang, Yulong; Zeng, Chaozhen

doi:10.1016/j.carbpol.2012.02.072

Cited by 57 publications

(38 citation statements)

References 18 publications

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“…As compared to a-CD and g-CD, b-CD is mostly preferred and widely used for complexation in pharmaceuticals 9 . The unique hollow truncated cone like structure of CDs with a hydrophobic cavity and hydrophilic wall make them capable of forming non-covalent inclusion complexes with guest molecules having suitable polarity and dimension 10,11 . Besides, parent b-CD, its hydrophilic derivatives hydroxypropyl-b-cyclodextrin and epichlorohydrinb-cyclodextrin (HP-b-CD and Epi-b-CD) are more effective in complexation.…”

Section: Introductionmentioning

confidence: 99%

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Gidwani

Vyas

2015

Drug Development and Industrial Pharmacy

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The objective of the present work was to investigate the inclusion behavior of bendamustine (BM) with β-cyclodextrin and its hydrophilic derivatives (HP-β-CD and Epi-β-CD) for the enhancement of aqueous solubility, dissolution and bioavailability. The supramolecular binary complexes were prepared by three different methods, viz. physical mixture (PM), kneading (KND) and co-evaporation (COE). Phase-solubility study revealed the higher solubilizing and complexing ability of polymerized cyclodextrin (Ks = 645 M(-1)) than parent cyclodextrin (Ks = 43 M(-1)) and chemically derived cyclodextrin (Ks = 100 M(-1)). Meanwhile, the solubility of BM was significantly enhanced in phosphate buffer of pH 6.8, which was 24.5 folds greater compared with the phosphate buffer pH 4.5 and four times greater than aqueous medium. The dissolution efficiency was found to be highest for BM: Epi-β-CD complex (87%) compared to BM: HP-β-CD complex (84%), BM: β-CD (79%) and pure drug (20%). In-vivo pharmacokinetic study revealed that the bioavailability of BM was enhanced 2.55 times on complexation with Epi-β-CD using KND method. The t1/2 of BM was increased from 34.2 min to approximately 75.7 min, allowing the absorption for longer time. The order of increase in solubility, dissolution and bioavailability of BM was KND > COE > PM > pure drug. Thus, the strategy of host-guest inclusion was very effective and could be successfully used in the development of suitable pharmaceutical dosage form with enhanced therapeutic activity.

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Section: Introductionmentioning

confidence: 99%

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Gidwani

Vyas

2015

Drug Development and Industrial Pharmacy

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“…Cyclodextrins (CDs) may help to overcome this problem [7]. Because of their cyclic structure, which presents a hydrophilic outer surface and a lipophilic central cavity, CDs are able to form inclusion complexes with certain lipophilic drugs increasing their aqueous solubility [8].…”

Section: Introductionmentioning

confidence: 99%

Gallic acid/hydroxypropyl-β-cyclodextrin complex: Improving solubility for application on in vitro/ in vivo Candida albicans biofilms

et al. 2017

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The aim of this study was to increase the solubility of gallic acid (GA) for the treatment of Candida albicans biofilm, which is very difficult to treat and requires high drug concentrations. Cyclodextrins (CDs) were used for this purpose. Complexes were evaluated by phase-solubility studies, prepared by spray drying and characterized by drug loading, scanning electron microscopy (SEM) and differential scanning calorimetry (DSC). The complexes were tested on C. albicans biofilm using in vitro and in vivo models. HPβCD formed soluble inclusion complexes with GA. The percentage of GA in GA/HPβCD was 10.8 ± 0.01%. The SEM and DSC analyses confirmed the formation of inclusion complexes. GA/HPβCD maintained the antimicrobial activity of the pure GA. GA/HPβCD was effective on C. albicans biofilms of 24 and 48h. The in vivo results showed an anti-inflammatory activity of GA/HPβCD with no difference in invading hypha counting among the groups. This study encourages the development of new antifungal agents.

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“…MBC, a broad spectrum benzimidazole fungicide, is usually used against fungi which affect crops, fruits and vegetables. However, MBC can be accumulated in plant and transferred to different parts, interfere mitosis of bacterial cell and inhibit its growth 14,15 . For example, Alicja Lewandowska et al found that MBC residue can be taken up by plants from extractable residue in soils 16 .…”

mentioning

confidence: 99%

“…Thus, the primary objective of this study is to evaluate the plant availability and phytotoxicity of MBC-BR after the amendment with SAP to Chinese cabbage seedlings. We planted the Chinese cabbage seed into the MBC-BR amended soil with HMBC, MBC-SAP and MBC treatment to reveal the effect of BR on the growth of Chinese cabbage by measuring the plant height, plant weight, tracing the 14 C content distribution and accumulation patterns in the different part of Chinese cabbage for safety assessment. Furthermore, we detected the BR release rate, extractable residue and bound residue in soil after the Chinese cabbage cultivation to demonstrate the soil safety.…”

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confidence: 99%

Phytoavailability of bound residue of Carbendazim to Chinese cabbage (Brassica campestris ssp.chinensis) coexisted with Superabsorbent polymers

Yang

Wang

et al. 2020

Sci Rep

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Understanding the bioavailability and phytotoxicity of carbendazim (MBc) bound residues (BR) in soils incubated with different Superabsorbent polymer (SAP) amendment on succeeding crops is essential to assess their environmental fate and risks. in our research, we studied the morphological characteristics and 14 c-accumulation of chinese cabbage and released BR in three typical cultivated soils. the plant dry weight was in order of superabsorbent-hydrogels formulations (HMBc) > MBc > MBC and SAP (MBC-SAP) at 35 d in basic soil 3 (S3), with 675.40 ± 29.07 mg/plant.d.w, 575.93 ± 25.35 mg/plant.d.w and 427.86 ± 18.79 mg/plant.d.w. The whole plant accumulated 2-fold more BR when grew in neutral soil 2 (S2) treated with SAP than MBC at 7 d. The root accumulated a greater proportion of 14 c-MBc residue than shoot, with order of MBC-SAP > MBc > HMBC at 21d. The results indicate MBC-BR could be released and accumulated in plant. HMBc promoted the chinese cabbage growth with lowest 14 c accumulation, while MBC-SAP inhibited plant growth with the highest 14 c uptake. the released BR rate was 61.43 ± 3.75% of initial BR in MBC-SAP, with 2-fold higher than MBC and HMBC. It is assumed HMBc could be a potential environmentally friendly measure for rational use of pesticides in future. Pesticides are ubiquitous chemicals in the environment, and are usually used to control crop disease and maintain the products. When pesticides are applied to the field and undergo degradation, their metabolites and they could bind to organic or mineral constituents of soil, and form the non-extractable residue (bound residue) in soil 1. Bound residue (BR) is generally regarded as the soil detoxification process, which involves chemicals could permanently bind to soil matrix, and are no longer bioavailable and bio-accessible to organisms. However, some studies reported that BR could be released via microbial activity and physic-chemical mechanism, and accumulated in living tissues and food webs, posing high threat to human health 2. Han et al. found 14 C-labeled residue of ZJ0273 was released from the BR-amended soil upon planting, and rice seedling took up the 14 C from soil contaminated with compound residues and was inhibited to grow 3. Gao et al. detected a clear uptake, accumulation and translocation of phenanthrene and pyrene by ryegrass, and significant phytoavailabilty of bound-PAH residue 4. Liu et al. also demonstrated that the earthworms accumulated 31.5% of the total radioactivity 14 C-BR-RM 5 after exposure to the BRs of 14 C-CYC. Thus, the food safety issue of agricultural products originated from contaminated soils should be given a public concern. The potential release, bioaccumulation and phytotoxicity of the BR to succeeding non-target organism are always important topics for understanding the environment and human food safety impact of pesticides. Soils are the vital resources that provide life-supporting services of food production, water cleaning and habits for human and wildlife. Intensified agricultural production has deter...

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Complexation of carbendazim with hydroxypropyl-β-cyclodextrin to improve solubility and fungicidal activity

Cited by 57 publications

References 18 publications

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Inclusion complexes of bendamustine withβ-CD, HP-β-CD and Epi-β-CD:in-vitroandin-vivoevaluation

Gallic acid/hydroxypropyl-β-cyclodextrin complex: Improving solubility for application on in vitro/ in vivo Candida albicans biofilms

Phytoavailability of bound residue of Carbendazim to Chinese cabbage (Brassica campestris ssp.chinensis) coexisted with Superabsorbent polymers

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