Development of chitosan nanocapsules for the controlled release of hexaconazole

Chauhan, Neetu; Dilbaghi, Neeraj; Gopal, Madhuban; Kumar, Rajesh; Kim, Ki‐Hyun; Kumar, Sandeep

doi:10.1016/j.ijbiomac.2016.12.059

Cited by 95 publications

(48 citation statements)

References 33 publications

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“…FTIR and DSC analysis confirmed the presence of bioactive compounds in the combined NF without any chemical interaction and amorphous nature of combined NF respectively. Moreover, the present study revealed that the NFs were less toxic to cell lines than pure drugs, as supported by the literature 35,36. In the present investigation, single NF doses showed less cytotoxicity compared to pure bioactive compounds.…”

Section: Discussionsupporting

confidence: 89%

<p>Antidiabetic activity enhancement in streptozotocin + nicotinamide–induced diabetic rats through combinational polymeric nanoformulation</p>

Rani

Dahiya

Dhingra

et al. 2019

IJN

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Background: The bioactive compounds glycyrrhizin (GL) and thymoquinone (TQ) have been reported for antidiabetic activity in pure and nanoformulation (NF) form. However, the antidiabetic effect of a combined nanoformulation of these two has not been reported in the literature. Here, a combinational nanomedicine approach was investigated to enhance the antidiabetic effects of the two bioactive compounds of GL and TQ (GT), in type 2 diabetic rats in reference to metformin. Methods: Two separately prepared NFs of GL (using polymeric nanoparticles) and TQ (using polymeric nanocapsules) were mixed to obtain a therapeutic cargo of nanomedicine and then characterized with respect to particle size, stability, morphology, chemical interaction, and in vivo behavior. Additionally, NFs were evaluated for their cytotoxic effect on Vero cell lines compared to the pure form. This nanomedicine was administered orally, both independently and in combination (pure form or NF) for 21 successive days to type 2 diabetic rats and the effect assessed in term of body weight, fasting blood-glucose level, and various biochemical parameters (such as lipid-profile parameters and HbA 1c ). Results: When these nanomedicines were applied in combined rather than individual forms, significant decreases in blood glucose and HbA 1c and significant improvements in body weight and lipid profile were observed, despite them containing lower amounts than the pure forms. The treatment of diabetic rats with GL and TQ, when administered independently in either pure or NF forms, did not lead to favorable trends in any studied parameters. Conclusion: The administration of combined GT NFs exhibited significant improvement in studied parameters. Improvements in antidiabetic activity could have been due to a synergistic effect of combined NFs, leading to enhanced absorption of NFs and lesser cytotoxic effects compared to pure bioactive compounds. Therefore, GT NFs demonstrated potential as a new medicinal agent for the management of diabetes.

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Section: Discussionsupporting

confidence: 89%

<p>Antidiabetic activity enhancement in streptozotocin + nicotinamide–induced diabetic rats through combinational polymeric nanoformulation</p>

Rani

Dahiya

Dhingra

et al. 2019

IJN

Self Cite

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“…Moreover, CHEN and CDEN also showed a nongenotoxic effect on the V79-4 hamster lung cells after 24 h exposure. However, early apoptosis (28.7%) was found in the 3T3 mouse fibroblast cells treated with CHEN for 48 h, whereas early apoptosis (52.4%) and late apoptosis (12.2%) were found in 3T3 mouse fibroblast cells treated with CDEN for 48 h. The result is in agreement with the work done by Chauhan et al, where the chitosan-hexaconazole nanocapsule reduced the cytotoxic effect on the Vero cell line compared to their commercial formulation and free hexaconazole [ 39 ]. In another work, Marayuma et al reported that the chitosan nanoencapsulation of herbicides (imazapic and imazapyr) reduced the cytotoxic and genotoxic effect on a hamster ovary cell line compared to free herbicides [ 40 ], hence proving the ability of chitosan nanocapsules as cytoprotective and genoprotective agents against toxic pesticides.…”

Section: Discussionsupporting

confidence: 89%

Cytoprotection, Genoprotection, and Dermal Exposure Assessment of Chitosan-Based Agronanofungicides

et al. 2020

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Health risks which result from exposure to pesticides have sparked awareness among researchers, triggering the idea of developing nanoencapsulation pesticides with the aim to enhance cytoprotection as well as genoprotection of the pesticides. In addition, nanocapsules of pesticides have slow release capability, high bioavailability, and site-specific delivery, which has attracted great interest from researchers. Hence, the objective of this work is to synthesize a nanoformulation of a fungicide of different sizes, namely, chitosan-hexaconazole nanoparticles (18 nm), chitosan-dazomet nanoparticles (7 nm), and chitosan-hexaconazole-dazomet nanoparticles (5 nm), which were then subjected to toxicological evaluations, including cytotoxicity, genotoxicity, cell death assay, and dermal irritation assays. Incubation of chitosan-based nanofungicides with V79-4 hamster lung cell did not reveal cytotoxicity or genotoxicity, potentially suggesting that encapsulation with chitosan reduces direct toxicity of the toxic fungicides. Meanwhile, pure fungicide revealed its high cytotoxic effect on V79-4 hamster lung cells. In addition, dermal exposure assessment on rabbits revealed that chitosan-hexaconazole nanoparticles are classified under corrosive subcategory 1C, while chitosan-dazomet nanoparticles are classified under corrosive subcategory 1B. Moreover, both chitosan-hexaconazole nanoparticles and chitosan-dazomet nanoparticles are classified as causing mild irritation.

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“…characterization of tQ-loaded nanocapsules. The particle size, PDI and zeta potential of the nanocapsules were measured using the Malvern Zetasizer nano ZS (Malvern Instruments Ltd, Malvern, UK) 64 at a scattering angle of 173°. A sample of 200 μl of the nanocapsules dispersion was diluted with deionized water and the particle size, PDI and zeta potential were measured at 25 °C.…”

Section: Synthesis Of Aa-conjugated Eudragit S100 Synthesis Of Tert-mentioning

confidence: 99%

Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors

Ramzy

Metwally

Nasr

et al. 2020

Sci Rep

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the biggest challenge in colorectal cancer therapy is to avoid intestinal drug absorption before reaching the colon, while focusing on tumor specific delivery with high local concentration and minimal toxicity. in our work, thymoquinone (tQ)-loaded polymeric nanocapsules were prepared using the nanoprecipitation technique using Eudragit S100 as polymeric shell. Conjugation of anisamide as a targeting ligand for sigma receptors overexpressed by colon cancer cells to Eudragit S100 was carried out via carbodiimide coupling reaction, and was confirmed by thin layer chromatography and 1 H-nMR. tQ nanocapsules were characterized for particle size, surface morphology, zeta potential, entrapment efficiency % (EE%), in vitro drug release and physical stability. A cytotoxicity study on three colon cancer cell lines (HT-29, HCT-116, Caco-2) was performed. Results revealed that the polymeric nanocapsules were successfully prepared, and the in vitro characterization showed a suitable size, zeta potential, EE% and physical stability. TQ exhibited a delayed release pattern from the nanocapsules in vitro. Anisamide-targeted tQ nanocapsules showed higher cytotoxicity against HT-29 cells overexpressing sigma receptors compared to their non-targeted counterparts and free TQ after incubation for 48 h, hence delineating anisamide as a promising ligand for active colon cancer targeting. Sigma receptors are expressed in normal cells of various organs including brain, kidney, liver, immune, endocrine and reproductive organ 1,2. Two distinguished subtypes were recognized and known as sigma-1 and sigma-2 3. Neurosteroids are the likely endogenous ligands for sigma-1 receptors 4 , and N,N-dimethyltryptamine; a natural alkaloid, was also found to be an endogenous ligand for sigma-1 receptors 5,6. A correlation between sigma receptors and diseases such as Parkinson's, Alzheimer's disease and cancer has been proposed 7 , and ligands for sigma-1 receptor were proven to improve various neurodegenerative disorders 8. Sigma-2 receptor is thought to be crucial for cell morphology, survival and differentiation 9. Sigma receptors are overexpressed in cancer cells of various organs 10 including cancers of the brain 11 , lung 12,13 , breast 14 , prostate gland 15 , kidney and colon 16. The tumor environment characterized by oxidative stress, hypoxia, low pH and insufficient supply of glucose and amino acids mediates disruption of endoplasmic reticulum protein folding. This in turn contributes to sigma-1 receptors activation to promote cell survival 7,17. In addition, sigma-2 receptors upregulation in cancerous tissues compared to healthy ones has been widely demonstrated 18,19. Benzamide derivatives demonstrate a high affinity towards sigma receptors 20-22. Anisamide (AA); a small molecular weight benzamide derivative was proven to exhibit high affinity for sigma receptors 23-25. In a review article previously published by our team the use of AA as a targeting ligand in several drug delivery systems was detailed 26. AA-functionalized doxorubicin-loade...

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Development of chitosan nanocapsules for the controlled release of hexaconazole

Cited by 95 publications

References 33 publications

<p>Antidiabetic activity enhancement in streptozotocin + nicotinamide–induced diabetic rats through combinational polymeric nanoformulation</p>

<p>Antidiabetic activity enhancement in streptozotocin + nicotinamide–induced diabetic rats through combinational polymeric nanoformulation</p>

Cytoprotection, Genoprotection, and Dermal Exposure Assessment of Chitosan-Based Agronanofungicides

Novel thymoquinone lipidic core nanocapsules with anisamide-polymethacrylate shell for colon cancer cells overexpressing sigma receptors

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