Nasal absorption in rats. II. Effect of enhancers on insulin absorption and nasal histology

Chandler, Susan G.; Ilium, Lisbeth; Thomas, N.W.

doi:10.1016/0378-5173(91)90344-n

Cited by 41 publications

(22 citation statements)

References 36 publications

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“…The nasal cavity has a comparatively large absorptive surface area and the high vascularity of the nasal mucosa makes sure that absorbed compounds are promptly distributed. Drugs absorbed into the affluent network of blood vessels get ahead directly into the systemic circulation in this manner circumventing hepatogastrointestinal first pass metabolism (Chandler et al, 1994;Illum, 2002;Costantino et al, 2007). The plasma pharmacokinetic profile after IN drug absorption for several drugs is comparable to that achieved with intravenous bolus injection (Duchateau et al, 1986a;Illum et al, 2002).…”

Section: Rationale For Commencing Nasal Delivery Of Therapeuticsmentioning

confidence: 83%

Nasal-nanotechnology: revolution for efficient therapeutics delivery

2014

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Context: In recent years, nanotechnology-based delivery systems have gained interest to overcome the problems of restricted absorption of therapeutic agents from the nasal cavity, depending upon the physicochemical properties of the drug and physiological properties of the human nose. Objective: The well-tolerated and non-invasive nasal drug delivery when combined with the nanotechnology-based novel formulations and carriers, opens the way for the effective systemic and brain targeting delivery of various therapeutic agents. To accomplish competent drug delivery, it is imperative to recognize the interactions among the nanomaterials and the nasal biological environment, targeting cell-surface receptors, drug release, multiple drug administration, stability of therapeutic agents and molecular mechanisms of cell signaling involved in patho-biology of the disease under consideration. Methods: Quite a few systems have been successfully formulated using nanomaterials for intranasal (IN) delivery. Carbon nanotubes (CNTs), chitosan, polylactic-co-glycolic acid (PLGA) and PLGA-based nanosystems have also been studied in vitro and in vivo for the delivery of several therapeutic agents which shown promising concentrations in the brain after nasal administration. Results and conclusion: The use of nanomaterials including peptide-based nanotubes and nanogels (NGs) for vaccine delivery via nasal route is a new approach to control the disease progression. In this review, the recent developments in nanotechnology utilized for nasal drug delivery have been discussed.

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Section: Rationale For Commencing Nasal Delivery Of Therapeuticsmentioning

confidence: 83%

Nasal-nanotechnology: revolution for efficient therapeutics delivery

2014

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“…Chandler et al, studied the effect of sodium taurodihydrofusidate (STDHF; a bile derivative), L-α lysophosphatidyl choline (LPC), polyoxyethylene-9-lauryl-ether (laureth 9) and diethylamine ethyl-dextran (DEAE-dextran) on nasal absorption of insulin in rat. [17] They found that all these enhancers increased insulin absorption with their ranking order being as follows: Laureth 9 > LPC = STDHF > DEAEdextran ≥ no enhancer. [17] The effect of sodium deoxycholate (SDC) on intranasal absorption of insulin was studied and the results showed that when insulin (0.5 IU/kg) in saline (pH 7.4) was administered without any absorption enhancer, no change in blood glucose level and insulin concentration was observed; however, blood glucose reduced in 10-20 min when 1% SDC was added to the insulin solution.…”

Section: Discussionmentioning

confidence: 99%

“…[17] They found that all these enhancers increased insulin absorption with their ranking order being as follows: Laureth 9 > LPC = STDHF > DEAEdextran ≥ no enhancer. [17] The effect of sodium deoxycholate (SDC) on intranasal absorption of insulin was studied and the results showed that when insulin (0.5 IU/kg) in saline (pH 7.4) was administered without any absorption enhancer, no change in blood glucose level and insulin concentration was observed; however, blood glucose reduced in 10-20 min when 1% SDC was added to the insulin solution. [18] The potency of bile salts in enhancing nasal absorption of insulin in human volunteers was ranked as deoxycholate > chenodeoxycholate > cholate > ursodeoxycholate.…”

Section: Discussionmentioning

confidence: 99%

Isolation, Characterization and Study of Enhancing Effects on Nasal Absorption of Insulin in Rat of the Total Saponin from Acanthophyllum squarrosum

Tabassi

Hosseinzadeh

Ramezani

et al. 2006

CDD

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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%

“…In developing oral insulin delivery systems with high bioavailability, several attempts have been explored to optimize insulin stability and absorption within the GIT (Chandler et al, 1994;Damge et al, 1995;Sarciaux et al, 1995;Iwanaga et al, 1997). Various approaches that could be adopted include modification of physicochemical properties such as lipophilicity and enzyme susceptibility, addition of novel function to macromolecules as well as the use of improved carrier system.…”

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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Nasal absorption in rats. II. Effect of enhancers on insulin absorption and nasal histology

Cited by 41 publications

References 36 publications

Nasal-nanotechnology: revolution for efficient therapeutics delivery

Nasal-nanotechnology: revolution for efficient therapeutics delivery

Isolation, Characterization and Study of Enhancing Effects on Nasal Absorption of Insulin in Rat of the Total Saponin from Acanthophyllum squarrosum

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

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