Background:The regulation of postprandial blood glucose concentration in a diabetic person is a toilsome task by the conventional approaches. The continuous monitoring and subcutaneous injection of insulin are always imperative for diabetes management. To overcome the hurdle associated with the conventional system, a glucose-responsive nanoparticle (NP)-based approach was developed for oral insulin administration. The objective of the work is the formulation and characterization of a nanocarrier-based bio-responsive, self-regulated oral insulin drug delivery system. Methods:The mannose ligand-conjugated NPs were prepared by the inotropic gelation method in which insulin and glucose oxidase enclosed alginate nanocarrier cross-linked by tripolyphosphate. The prepared NPs were filled into the enteric-coated capsule and their release profile was determined at different pH and glucose concentrations. NPs were characterized by size distribution, % drug entrapment, enzyme activity, and in vivo and in vitro drug release studies. Results:The average size, surface potential, % drug entrapment of optimized NPs were 245.52 ± 3.37 nm, 22.12 ± 2.13, and 76.15±1.3%, respectively. The release of insulin from optimized NPs (GOx-ALG-MCNPs) (98.56±0.06%) occurs only at higher sugar concentrations (≥ 400 mg/dL) and prevents the release at low sugar concentrations (< 100 mg/dL). The enteric capsule shell protected the formulation to the gastric environment upon oral administration and directed them into the intestine. Mucoadhesion characteristics of NPs prolonged intestinal retention to make them available for cellular uptake. Glucose sensitivity and glucose-dependent effect on different pH environments study revealed that NPs released the drug only at higher concentrations of sugar solution while inhibiting the release at normal and lower sugar concentrations. Besides, compared to other prepared formulations, the GOx-ALG-MCNPs displayed controlled insulin release in response to glucose concentration.Conclusions: An important finding of GOx-ALG-MCNPs is autoregulating, glucose-responsive behavior imparting a significantly controlled lowering of blood glucose in an animal model. The findings reveal that the developed glucose-responsive NPs may prove to be a potential strategy for oral insulin delivery.
The primary objective of the proposed research work is to extract and enrich pure andrographolide (AGL) by varying the polarity index and Hildebrand solubility parameter (δ) of a moderately polar solvent. Both parameters affect the solubility of AGL in different solvents and extraction methods. AGL was extracted from the whole plant Andrographis paniculata. Continuous or Direct, Maceration and Soxhlet extraction method used for extraction. Based on the appearance of the crystal in the direct Soxhlet ethyl acetate method, their yield was further optimized by using a randomized response surface (RSM) and quadratic model-based Box‒Behnken design (BBD). HPTLC was used to determine the AGL extraction efficiency, purity, and quantification. Based on the obtained result, the pure andrographolide crystal (yield 0.185 g/g) was obtained by direct Soxhlet extraction. Ethyl acetate is used as a solvent. The Rf exhibited in the TLC chromatogram was 0.28. The FT-IR spectra exhibited characteristic peaks similar to the standard AGL, and 1H-NMR and 13C NMR elucidated the crystal structure. The DEPT − 90/135 spectra showed that the extracted crystal was pure AGL. One of the novel approaches is isolating pure AGL crystals in a moderately polar solvent (ethyl acetate) by elevating the Hildebrand solubility parameter despite using polar solvents. AGL crystals were obtained from direct Soxhlet extraction by ethyl acetate. It is a single-step and more economical method. It can be easily transformed into a pilot or industrial setup to extract the pure AGL.
The primary objective of the proposed research work is to extract and enrich the pure Andrographolide (AGL) by varying the polarity index and Hildebrand solubility parameter (δ) of a moderately polar solvent. Both parameters affect the solubility of AGL in different solvents and extraction methods. AGL was extracted from the whole plant of Andrographis paniculata. Continuous or Direct, Maceration and Soxhlet extraction method used for extraction. Based on the appearance of the crystal in the Direct Soxhlet Ethyl acetate method, their yield was further optimized by using a Randomized response surface (RSM), Quadratic model-based Box-Behnken design (BBD). The HPTLC performed the AGL extraction efficiency, purity, and quantification. Based on the obtained result, the pure Andrographolide crystal (yield 0.185 g/g) was obtained by Direct Soxhlet extraction. Ethyl acetate is used as a solvent. Rf exhibited in the TLC chromatogram was 0.28. FT-IR spectra exhibited characteristics peak similar to the standard AGL, and 1H-NMR, 13C NMR elucidated crystal structure. DEPT -90/135 spectra depicted that extracted crystal was pure AGL. It is one of the novel approaches to isolating pure AGL crystal in a moderately polar solvent (Ethyl acetate) by elevating the Hildebrand solubility parameter despite using polar solvents. AGL crystal was obtained from Direct Soxhlet extraction by Ethyl acetate. It is a single-step and more economical method. It can be easily transformed into a pilot or industrial setup to extract Pure AGL.
The primary objective of the proposed research work is to extract and enrich the pure Andrographolide (AGL) by varying the polarity index and Hildebrand solubility parameter (δ) of a moderately polar solvent. Both parameters affect the solubility of AGL in different solvents and extraction methods. AGL was extracted from the whole plant of Andrographis paniculata. Continuous or Direct, Maceration and Soxhlet extraction method used for extraction. Based on the appearance of the crystal in the Direct Soxhlet Ethyl acetate method, their yield was further optimized by using a Randomized response surface (RSM), Quadratic model-based Box-Behnken design (BBD). The HPTLC performed the AGL extraction efficiency, purity, and quantification. Based on the obtained result, the pure Andrographolide crystal (yield 0.185 g/g) was obtained by Direct Soxhlet extraction. Ethyl acetate is used as a solvent. Rf exhibited in the TLC chromatogram was 0.28. FT-IR spectra exhibited characteristics peak similar to the standard AGL, and 1H-NMR, 13C NMR elucidated crystal structure. DEPT − 90/135 spectra depicted that extracted crystal was pure AGL. It is one of the novel approaches to isolating pure AGL crystal in a moderately polar solvent (Ethyl acetate) by elevating the Hildebrand solubility parameter despite using polar solvents. AGL crystal was obtained from Direct Soxhlet extraction by Ethyl acetate. It is a single-step and more economical method. It can be easily transformed into a pilot or industrial setup to extract Pure AGL.
scite is a Brooklyn-based organization that helps researchers better discover and understand research articles through Smart Citations–citations that display the context of the citation and describe whether the article provides supporting or contrasting evidence. scite is used by students and researchers from around the world and is funded in part by the National Science Foundation and the National Institute on Drug Abuse of the National Institutes of Health.
hi@scite.ai
10624 S. Eastern Ave., Ste. A-614
Henderson, NV 89052, USA
Copyright © 2024 scite LLC. All rights reserved.
Made with 💙 for researchers
Part of the Research Solutions Family.