Cyclodextrin–insulin complex encapsulated polymethacrylic acid based nanoparticles for oral insulin delivery

Sajeesh, S.; Sharma, Chandra P.

doi:10.1016/j.ijpharm.2006.06.019

Cited by 227 publications

(91 citation statements)

References 35 publications

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“…Insulin administered via the oral route will help eliminate the pain caused by injection, psychological barriers associated with multiple daily injections, such as needle anxiety (Korytkowski, 2002) and possible infections (Lin et al, 2007). However, being a protein, it undergoes rapid enzymatic degradation in the stomach, inactivation and digestion by proteolytic enzymes in the intestinal lumen (Patki & Jagasia, 1996;Agarwal & Khan, 2001, Nakamura et al, 2004Jain et al, 2005;Sajeesh & Sharma 2006). Another major barrier to the absorption of hydrophilic macromolecules like insulin is that they cannot diffuse across epithelial cells through lipid-bilayer cell membranes to the blood stream (Lin et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

Ansari¹,

Anwer²,

Jamil³

et al. 2015

Drug Delivery

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Objective: Insulin is a hormone used in the treatment of diabetes mellitus. Multiple injections of insulin every day may causes pain, allergic reactions at injection site, which lead to low patient compliance. The aim of this work was to develop and evaluate an efficient solid lipid nanoparticle (SLN) carrier for oral delivery of insulin. Methods: SLNs were prepared by double emulsion solvent evaporation (w/o/w) technique, employing glyceryltrimyristate (Dynasan 114) as lipid phase and soy lecithin and polyvinyl alcohol as primary and secondary emulsifier, respectively, and evaluated in vitro for particle size, polydispersity index (PDI) and drug entrapment. Results: Among the eight different developed formulae (F1-F8), F7 showed an average particle size (99 nm), PDI (0.021), high entrapment of drug (56.5%). The optimized formulation (F7) was further evaluated by FT-IR, DSC, XRD, in vitro release, permeation, stability, bioavailability and pharmacological studies. Insulin-loaded SLNs showed better protection from gastrointestinal environment as evident from the relative bioavailability, which was enhanced five times as compared to the insulin solution. A significant enhancement of relative bioavailability of insulin was observed, i.e. approximately five times of pure insulin solution when loaded in SLN (8.26% versus 1.7% only).

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Section: Introductionmentioning

confidence: 99%

Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

Ansari¹,

Anwer²,

Jamil³

et al. 2015

Drug Delivery

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“…Finally, unreacted monomers are removed by dialysis or subsequent washes of the formed particles with distilled water. Nanoparticles obtained by this method have been used to administer insulin, bovine serum albumin and silk peptide through the oral route (Hu et al 2002, Sajeesh and Sharma 2006a, Sajeesh and Sharma 2006b). …”

Section: Modified Ionic Gelation With Radical Polymerisationmentioning

confidence: 99%

“…Chitosan, alginate, arabic gum, carboxymethyl cellulose, carrageenan, chondroitin sulfate, cyclodextrins, dextran sulfate, polyacrylic acid, poly-γ-glutamic acid, insulin, DNA (Erbacher et al 1998, Hu et al 2002, Du et al 2004, Sarmento et al 2006a, Sarmento et al 2006b, Lin et al 2007, Bayat et al 2008, Lin et al 2008, Teijeiro-Osorio et al 2009, Avadi et al 2010, Grenha et al 2010b, Kaihara et al 2011, Yeh et al 2011 Modified ionic gelation with radical polymerisation Chitosan, acrylic acid, methacrylic acid, polyethylene glycol, polyether (Hu et al 2002, Sajeesh and Sharma 2006a, Sajeesh and Sharma 2006b Desolvation Chitosan (Mao et al 2001, Borges et al 2005 Targeting 1 2 3 4 5 6 7 8 9 10 11 12 13 14 15 16 17 18 19 20 ...…”

Section: Declaration Of Interestmentioning

confidence: 99%

Chitosan nanoparticles: a survey of preparation methods

Grenha¹

2012

Journal of Drug Targeting

236

140

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The application of macromolecules in therapy is frequently hindered by stability and/or permeation issues. These limitations have been addressed by the pharmaceutical industry through the development of suitable non-injectable drug carriers. In this context, nanoparticles have emerged as one of the most exciting tools, due to the increased surface-to-volume ratio, which provides an intimate interaction with epithelial surfaces. Nanoparticles further enable the encapsulated molecules to retain their biological activity, from the production steps to the final release. Chitosan has reached a prominent position as carrier-forming material, as diverse methods can be applied to produce nanoparticles using that excipient. These involve either hydrophilic or lipophilic environments that generally result in mild conditions or aggressive and time-consuming processes, respectively. In this review, a detailed description of methods employed to produce chitosan nanocarriers is provided, accompanied by illustrative schemes of the procedures. The emphasis is on the variables reported to affect the final properties of the vehicles.3

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“…Figure 4 also shows a slight reduction in blood glucose level after oral administration of insulin solution. It is quite improbable for insulin absorption to occur in the stomach (Chandler et al, 1994;Damage et al, 1995;Sarciaux et al, 1995;Iwanaga et al, 1997;Krauland et al, 2004;Li & Deng, 2004;Nakamura et al, 2004;Sajeesh & Sharma, 2006;Lin, 2007); thus the reduction in the blood glucose could be due to some of the insulin solution reaching the intestine since high doses of insulin solution were administered to the rats. Blood glucose reduction occurred within 30 min of oral administration in some samples.…”

Section: Blood Glucose Reducing Efficiencymentioning

confidence: 99%

“…The oral route is considered to be the most convenient, acceptable and desired route of drug delivery which will help eliminate the pain caused by injection, psychological barrier associated with multiple daily injection and possible infections (Kisel et al, 2001;Kim & Peppas, 2003;Whitehead et al, 2004;Cui et al, 2006;Sarmento et al, 2007). Oral delivery of insulin as a non-invasive therapy for diabetes mellitus is still a challenge to the drug delivery technology, due to low oral bioavailability, lack of lipophility, poor permeability across intestinal epithelium because of insulin high molecular weight as well as digestion by proteolytic enzymes in the luminal cavity (Tozaki, 2001; Gowthamarajan & Kulkarni, 2003;Tiyaboonchai, 2003;Krauland et al, 2004;Li & Deng, 2004;Nakamura et al, 2004;Toorisaka et al, 2005;Sajeesh & Sharma, 2006;Sarmento, 2006;Tuesca & Lowman, 2006;Lin, 2007;Simon, 2007).…”

Section: Introductionmentioning

confidence: 99%

Influence of magnesium stearate on the physicochemical and pharmacodynamic characteristics of insulin-loaded Eudragit entrapped mucoadhesive microspheres

et al. 2014

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Effective oral insulin delivery has remained a challenge to the pharmaceutical industry. This study was designed to evaluate the effect of magnesium stearate on the properties of insulin-loaded Eudragit Õ RL 100 entrapped mucoadhesive microspheres. Microspheres containing Eudragit Õ RL 100, insulin, and varying concentrations of magnesium stearate (agglomeration-preventing agent) were prepared by emulsification-coacervation method and characterized with respect to differential scanning calorimetry (DSC), morphology, particle size, loading efficiency, mucoadhesive and micromeritics properties. The in vitro release of insulin from the microspheres was performed in simulated intestinal fluid (SIF, pH 7.2) while the in vivo hypoglycemic effect was investigated by monitoring the plasma glucose level of the alloxaninduced diabetic rats after oral administration. Stable, spherical, brownish, mucoadhesive, discrete and free flowing insulin-loaded microspheres were formed. While the average particle size and mucoadhesiveness of the microspheres increased with an increase in the proportion of magnesium stearate, loading efficiency generally decreased. After 12 h, microspheres prepared with Eudragit Õ RL 100: magnesium stearate ratios of 15:1, 15:2, 15:3 and 15:4 released 68.20 ± 1.57, 79.40 ± 1.52, 76.60 ± 1.93 and 70.00 ± 1.00 (%) of insulin, respectively. Reduction in the blood glucose level for the subcutaneously (sc) administered insulin was significantly (p 0.05) higher than for most of the formulations. However, the blood glucose reduction effect produced by the orally administered insulin-loaded microspheres prepared with four parts of magnesium stearate and fifteen parts of Eudragit Õ RL 100 after 12 h was equal to that produced by subcutaneously administered insulin solution. The results of this study can suggest that this carrier system could be an alternative for the delivery of insulin.

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Cyclodextrin–insulin complex encapsulated polymethacrylic acid based nanoparticles for oral insulin delivery

Cited by 227 publications

References 35 publications

Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

Enhanced oral bioavailability of insulin-loaded solid lipid nanoparticles: pharmacokinetic bioavailability of insulin-loaded solid lipid nanoparticles in diabetic rats

Chitosan nanoparticles: a survey of preparation methods

Influence of magnesium stearate on the physicochemical and pharmacodynamic characteristics of insulin-loaded Eudragit entrapped mucoadhesive microspheres

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