Challenges and advances in nanoparticle-based oral insulin delivery

Rekha, M.R.; Sharma, Chandra P.

doi:10.1586/erd.09.43

Cited by 62 publications

(37 citation statements)

References 83 publications

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“…In contrast, correspondingly, no intact insulin and 3.14±2.55% of intact insulin in solution could be detected. These results confirmed earlier studies HA nanoparticles could protect insulin against protease enzymes to a certain extent in GI tract as others polymeric nanoparticles did (26). It was likely attributed to the entrapment of insulin in nanoparticles and then shielding it from enzyme digestion.…”

Section: Ha Nanoparticles Protecting Insulin Against Enzymatic Degradsupporting

confidence: 91%

Insulin-Loaded pH-Sensitive Hyaluronic Acid Nanoparticles Enhance Transcellular Delivery

et al. 2012

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Abstract. In the present study, we developed novel insulin-loaded hyaluronic acid (HA) nanoparticles for insulin delivery. The insulin-loaded HA nanoparticles were prepared by reverse-emulsion-freeze-drying method. This method led to a homogenous population of small HA nanoparticles with average size of 182.2 nm and achieved high insulin entrapment efficiencies (approximately 95%). The pH-sensitive HA nanoparticles as an oral delivery carrier showed advantages in protecting insulin against the strongly acidic environment of the stomach, and not destroying the junction integrity of epithelial cells which promise long-term safety for chronic insulin treatment. The results of transport experiments suggested that insulinloaded HA nanoparticles were transported across Caco-2 cell monolayers mainly via transcellular pathway and their apparent permeability coefficient from apical to basolateral had more than twofold increase compared with insulin solution. The efflux ratio of P app (B to A) to P app (A to B) less than 1 demonstrated that HA nanoparticle-mediated transport of insulin across Caco-2 cell monolayers underwent active transport. The results of permeability through the rat small intestine confirmed that HA nanoparticles significantly enhanced insulin transport through the duodenum and ileum. Diabetic rats treated with oral insulin-loaded HA nanoparticles also showed stronger hypoglycemic effects than insulin solution. Therefore, these HA nanoparticles could be a promising candidate for oral insulin delivery.

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Section: Ha Nanoparticles Protecting Insulin Against Enzymatic Degradsupporting

confidence: 91%

Insulin-Loaded pH-Sensitive Hyaluronic Acid Nanoparticles Enhance Transcellular Delivery

et al. 2012

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“…Nanocarrier systems have gained constantly increasing interest in last two decades in order to overcome the major challenges being associated with oral administration, namely poor solubility, poor GI stability and poor permeability. Among the systems, polymeric nanoparticles (NPs) have been extensively applied to conquer these drawbacks because of their ability to prevent the active ingredients from chemical and enzymatic degradation in GI tract (Cartiera et al, 2009;Ramesan & Sharma, 2009), facilitate the intestinal absorption of drugs, while ease of processing, readily control of their physicochemical properties.…”

Section: Introductionmentioning

confidence: 99%

Effects of borneol on the pharmacokinetics of 9-nitrocamptothecin encapsulated in PLGA nanoparticles with different size via oral administration

Han

Qing

et al. 2016

Drug Delivery

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Context: Although nanocarriers provide promising potential for oral drug delivery, the delivery efficiency remains unsatisfactory and needs to be improved. Size is considered to be the most important characteristic of nanoparticles related to their oral absorption. Borneol has been proved to have the ability to enhance the penetration and transport of many drugs through various physical barriers. Objective: To investigate the effect of the particle size and coadministration of borneol on the pharmacokinetics and bioavailability of entrapped drug in different size poly(lactic-co-glycolic acid) (PLGA) nanoparticles. Materials and methods: 9-Nitrocamptothecin (9-NC)-loaded PLGA nanoparticles with three different range of size (50-100 nm, 100-200 nm, 200-300 nm) were prepared by emulsion solvent-evaporation method. The pharmacokinetic study in rats of these nanoparticles with borneol was carried out. Results:The experiments showed that the encapsulation drug in nanoparticles with size below 200 nm could improve the oral bioavailability of 9-NC. The small size nanoparticles (50-100 nm) had a better improvement efficacy. As for borneol, it played a significant promotion effect only on the small nanoparticles. Moreover, there was no significant influence on the nanoparticles with size more than 100 nm. Discussion and conclusion: The study indicated that both entrapping drug in nanoparticles with the size below 100 nm and coadministrating with borneol could enhance the gastrointestinal absorption of water insoluble drug. The combination of the two strategies provides a potential approach to improve the oral bioavailability of drug.

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“…2 Approaches taken to improve their oral bioavailability have included protecting against enzymatic degradation and increasing permeability and absorption time. 1,[3][4][5] In recent decades, lipid emulsions (such as water in oil [w/o] microemulsions 6 and multiple emulsions) have been widely used in the enhancement of the oral bioavailability of peptides and proteins 7,8 due to their protective ability; improving the fluidity of membrane and transient opening the tight junctions induced by lipid constituents or surfactants. 9,10 After oral administration w/o microemulsions are easily transformed into oil in water (o/w) emulsions in the gastric juices.…”

Section: Introductionmentioning

confidence: 99%

Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats

Li¹,

Qi²,

Xie³

et al. 2012

IJN

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This study aimed to prepare nanoemulsions coated with alginate/chitosan for oral insulin delivery. Uncoated nanoemulsions were prepared by homogenization of a water in oil in water (w/o/w) multiple emulsion that was composed of Labrafac ® CC, phospholipid, Span™ 80 and Cremorphor ® EL. Coating of the nanoemulsions was achieved based on polyelectrolyte cross-linking, with sequential addition of calcium chloride and chitosan to the bulk nanoemulsion dispersion that contained alginate. The particle size of the coated nanoemulsions was about 488 nm and the insulin entrapment ratio was 47.3%. Circular dichroism spectroscopy proved conformational stability of insulin against the preparative stress. In vitro leakage study indicated well-preserved integrity of the nanoemulsions in simulated gastric juices. Hypoglycemic effects were observed in both normal and diabetic rats. The relative pharmacological bioavailability of the coated nanoemulsion with 25 and 50 IU/kg insulin were 8.42% and 5.72% in normal rats and 8.19% and 7.84% in diabetic rats, respectively. Moreover, there were significantly prolonged hypoglycemic effects after oral administration of the coated nanoemulsions compared with subcutaneous (sc) insulin. In conclusion, the nanoemulsion coated with alginate/chitosan was a potential delivery system for oral delivery of polypeptides and proteins.

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Challenges and advances in nanoparticle-based oral insulin delivery

Cited by 62 publications

References 83 publications

Insulin-Loaded pH-Sensitive Hyaluronic Acid Nanoparticles Enhance Transcellular Delivery

Insulin-Loaded pH-Sensitive Hyaluronic Acid Nanoparticles Enhance Transcellular Delivery

Effects of borneol on the pharmacokinetics of 9-nitrocamptothecin encapsulated in PLGA nanoparticles with different size via oral administration

Nanoemulsions coated with alginate/chitosan as oral insulin delivery systems: preparation, characterization, and hypoglycemic effect in rats

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