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Novel PLGA-based nanoparticles for the oral delivery of insulin.

Malathi S, Nandhakumar P, Pandiyan V, Webster TJ, Balasubramanian S - Int J Nanomedicine (2015)

Bottom Line: The serum glucose level was significantly (twofold) decreased on treatment with ISTPPLG NPs, and there was a threefold decrease with insulin-loaded PLGA (70/30) NPs when compared to that of free insulin-treated diabetic rats.The results show that the oral administration of ISTPPLG6 NPs is an effective method of reducing serum glucose level for a period of 24 hours.Histopathological studies reveal that ISTPPLG NPs could restore the damage caused by streptozotocin in the liver, kidneys, and pancreas, indicating its biocompatibility and regenerative effects.

View Article: PubMed Central - PubMed

Affiliation: Department of Inorganic Chemistry, Guindy Campus, University of Madras, Chennai, Tamil Nadu, India.

ABSTRACT

Background: Insulin is the drug therapy for patients with insulin-dependent diabetes mellitus. A number of attempts have been made in the past to overcome the problems associated with the oral delivery of insulin, but with little success. Orally administered insulin has encountered with many difficulties such as rapid degradation and poor intestinal absorption. The potential use of D-α-tocopherol poly(ethylene glycol) 1000 succinate (TPGS)-emulsified poly(ethylene glycol) (PEG)-capped poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) was investigated for sustained delivery of insulin (IS).

Objective: To investigate the efficacy of TPGS-emulsified PEG-capped PLGA NPs (TPPLG NPs) as a potential drug carrier for the oral delivery of insulin.

Methods: A series of biodegradable low-molecular-weight PLGA (80/20 [PLG4] and 70/30 [PLG6]) copolymers were synthesized by melt polycondensation. The commercial insulin-loaded TPGS-emulsified PEG-capped PLGA NPs (ISTPPLG NPs) were synthesized by water-oil-water emulsion solvent evaporation method. The physical and chemical properties of PLGA copolymers, particle size, zeta potential, and morphology of the NPs were examined. The in vivo studies of ISTPPLG NPs were carried out in diabetic rats by oral administration.

Results: The maximum encapsulation efficiency of ISTPPLG6 NPs was 78.6% ± 1.2%, and the mean diameter of the NPs was 180 ± 20 nm. The serum glucose level was significantly (twofold) decreased on treatment with ISTPPLG NPs, and there was a threefold decrease with insulin-loaded PLGA (70/30) NPs when compared to that of free insulin-treated diabetic rats. The results show that the oral administration of ISTPPLG6 NPs is an effective method of reducing serum glucose level for a period of 24 hours. Histopathological studies reveal that ISTPPLG NPs could restore the damage caused by streptozotocin in the liver, kidneys, and pancreas, indicating its biocompatibility and regenerative effects.

Conclusion: ISTPPLG6 NPs can act as potential drug carriers for the oral delivery of insulin.

No MeSH data available.


Related in: MedlinePlus

Effect of ISTPPLG6 NPs on histopathological changes of the liver, kidney, and pancreas.Abbreviation: ISTPPLG6 NPs, insulin-loaded tocopherol poly(ethylene glycol) 1000 succinate-emulsified poly(ethylene glycol)-capped poly(lactic-co-glycolic acid) (68/32) nanoparticles.
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f7-ijn-10-2207: Effect of ISTPPLG6 NPs on histopathological changes of the liver, kidney, and pancreas.Abbreviation: ISTPPLG6 NPs, insulin-loaded tocopherol poly(ethylene glycol) 1000 succinate-emulsified poly(ethylene glycol)-capped poly(lactic-co-glycolic acid) (68/32) nanoparticles.

Mentions: The histopathological studies were carried out 12 hours after the oral administration of ISTPPLG NPs. Liver sections of diabetic control rats showed marked microscopical changes such as hydropic degeneration of hepatocytes and dilatation of sinusoids when compared to that of normal control rats. The treatment with ISTPPLG6 NPs diminished the intensity of degeneration and dilatation of sinusoids. The microscopic examination of diabetic control rats (kidney) showed marked changes such as tubular epithelial cell degeneration and cystic dilatation of tubules. The treatment with ISTPPLG6 NPs reduced the intensity of degeneration and cystic dilatation of tubules. The pancreatic sections of diabetic control and insulin-treated and ISTPPLG6 NPs-treated diabetic groups showed marked microscopical changes such as atrophy and reduction in the number of islet cells (Figure 7).


Novel PLGA-based nanoparticles for the oral delivery of insulin.

Malathi S, Nandhakumar P, Pandiyan V, Webster TJ, Balasubramanian S - Int J Nanomedicine (2015)

Effect of ISTPPLG6 NPs on histopathological changes of the liver, kidney, and pancreas.Abbreviation: ISTPPLG6 NPs, insulin-loaded tocopherol poly(ethylene glycol) 1000 succinate-emulsified poly(ethylene glycol)-capped poly(lactic-co-glycolic acid) (68/32) nanoparticles.
© Copyright Policy
Related In: Results  -  Collection

License
Show All Figures
getmorefigures.php?uid=PMC4383223&req=5

f7-ijn-10-2207: Effect of ISTPPLG6 NPs on histopathological changes of the liver, kidney, and pancreas.Abbreviation: ISTPPLG6 NPs, insulin-loaded tocopherol poly(ethylene glycol) 1000 succinate-emulsified poly(ethylene glycol)-capped poly(lactic-co-glycolic acid) (68/32) nanoparticles.
Mentions: The histopathological studies were carried out 12 hours after the oral administration of ISTPPLG NPs. Liver sections of diabetic control rats showed marked microscopical changes such as hydropic degeneration of hepatocytes and dilatation of sinusoids when compared to that of normal control rats. The treatment with ISTPPLG6 NPs diminished the intensity of degeneration and dilatation of sinusoids. The microscopic examination of diabetic control rats (kidney) showed marked changes such as tubular epithelial cell degeneration and cystic dilatation of tubules. The treatment with ISTPPLG6 NPs reduced the intensity of degeneration and cystic dilatation of tubules. The pancreatic sections of diabetic control and insulin-treated and ISTPPLG6 NPs-treated diabetic groups showed marked microscopical changes such as atrophy and reduction in the number of islet cells (Figure 7).

Bottom Line: The serum glucose level was significantly (twofold) decreased on treatment with ISTPPLG NPs, and there was a threefold decrease with insulin-loaded PLGA (70/30) NPs when compared to that of free insulin-treated diabetic rats.The results show that the oral administration of ISTPPLG6 NPs is an effective method of reducing serum glucose level for a period of 24 hours.Histopathological studies reveal that ISTPPLG NPs could restore the damage caused by streptozotocin in the liver, kidneys, and pancreas, indicating its biocompatibility and regenerative effects.

View Article: PubMed Central - PubMed

Affiliation: Department of Inorganic Chemistry, Guindy Campus, University of Madras, Chennai, Tamil Nadu, India.

ABSTRACT

Background: Insulin is the drug therapy for patients with insulin-dependent diabetes mellitus. A number of attempts have been made in the past to overcome the problems associated with the oral delivery of insulin, but with little success. Orally administered insulin has encountered with many difficulties such as rapid degradation and poor intestinal absorption. The potential use of D-α-tocopherol poly(ethylene glycol) 1000 succinate (TPGS)-emulsified poly(ethylene glycol) (PEG)-capped poly(lactic-co-glycolic acid) (PLGA) nanoparticles (NPs) was investigated for sustained delivery of insulin (IS).

Objective: To investigate the efficacy of TPGS-emulsified PEG-capped PLGA NPs (TPPLG NPs) as a potential drug carrier for the oral delivery of insulin.

Methods: A series of biodegradable low-molecular-weight PLGA (80/20 [PLG4] and 70/30 [PLG6]) copolymers were synthesized by melt polycondensation. The commercial insulin-loaded TPGS-emulsified PEG-capped PLGA NPs (ISTPPLG NPs) were synthesized by water-oil-water emulsion solvent evaporation method. The physical and chemical properties of PLGA copolymers, particle size, zeta potential, and morphology of the NPs were examined. The in vivo studies of ISTPPLG NPs were carried out in diabetic rats by oral administration.

Results: The maximum encapsulation efficiency of ISTPPLG6 NPs was 78.6% ± 1.2%, and the mean diameter of the NPs was 180 ± 20 nm. The serum glucose level was significantly (twofold) decreased on treatment with ISTPPLG NPs, and there was a threefold decrease with insulin-loaded PLGA (70/30) NPs when compared to that of free insulin-treated diabetic rats. The results show that the oral administration of ISTPPLG6 NPs is an effective method of reducing serum glucose level for a period of 24 hours. Histopathological studies reveal that ISTPPLG NPs could restore the damage caused by streptozotocin in the liver, kidneys, and pancreas, indicating its biocompatibility and regenerative effects.

Conclusion: ISTPPLG6 NPs can act as potential drug carriers for the oral delivery of insulin.

No MeSH data available.


Related in: MedlinePlus