Liposomes with phosphatidylethanol as a carrier for oral delivery of insulin: studies in the rat

Kisel, M. A.; Kulik, Liudmila; Tsybovsky, Iosif S.; Vlasov, Alexander P.; Vorob'yov, M.S.; Kholodova, Elena; Zabarovskaya, Z.V.

doi:10.1016/s0378-5173(01)00579-8

Cited by 146 publications

(64 citation statements)

References 29 publications

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“…Blood glucose reduction occurred within 30 min of oral administration in some samples. This could be attributed to such factors as early gastric emptying of the drug from the stomach into the small intestine and the effective mucoadhesiveness of the polymer matrix (Eudragit Õ RL 100) that was efficient in adhering the microspheres to the gastric mucosa and protecting the insulin from degradation which is one of the major drawbacks in oral insulin delivery (Beals & Kovach, 1997;Kisel et al, 2001;Owens, 2002;Giriraj & Giriraj, 2003;Gowthamarajan & Kulkarni, 2003;Kim & Peppas, 2003;Whitehead et al, 2004;Cui et al, 2006;Morishita & Peppas, 2006;Sarmento et al, 2007;Pamnani, 2008). It was helpful to protect insulin activity against the enzymatic attack in harsh environment of stomach and intestine.…”

Section: Blood Glucose Reducing Efficiencymentioning

confidence: 99%

“…Insulin is administered parenterally by subcutaneous injection (Beals & Kovach, 1997), which results in low level of compliance due to pain as well as complications due to multiple jabs, hence the need for an alternative less invasive but effective method of insulin administration (Gowthamarajan & Kulkarni, 2003). 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%

“…The successful production of an effective oral insulin formulation will depend on the development of an appropriate drug delivery (carrier) system that will protect insulin from the degradative effect of enzymes and pH of the GIT (Caliceti & Veronese, 1999). The use of carrier systems, such as liposomes, mixed micelles, multiple emulsions, microemulsions, microspheres, hydrogels, azopolymer coating, site specific drug delivery systems, absorption enhancers, enzyme inhibitors and modifications of chemical structure have been shown to improve the gastrointestinal absorption of peptide drugs (Yamamoto et al, 1994;Tozaki et al, 1997;Chetty & Chien, 1998;Caliceti & Veronese, 1999;Kisel et al, 2001).…”

Section: Introductionmentioning

confidence: 99%

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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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Section: Blood Glucose Reducing Efficiencymentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

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

et al. 2014

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“…The application of polar lipids in other industrial fields includes uses as a drug delivery carrier and as fat liquoring for leather fatting, etc. [Guo et al, 2005;Kisel et al, 2001;Vannieuwenhuyzen, 1981]. In contrast with the polar lipid fraction of plants, dairy products contain a substantial part of sphingolipids, which can be used as raw material for the production of ceramides, applicable in the cosmetic industry [Becart et al, 1990].…”

Section: Functionalities and Applications Of Mfgmmentioning

confidence: 99%

Composition, Properties and Nutritional Aspects of Milk Fat Globule Membrane – A Review

El-Loly¹

2011

Pol. J. Food Nutr. Sci.

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processes and defense mechanisms in the newborn [Cavaletto et al., 2006].The stabilizing membrane acts as reactive sorts on the interface between the barriers of milk serum. As such, it can be globule and rate-controlling for a host of physical and of enzymes chemical interactions, e.g., binding mace elements; controlled release of the polar materials products of lipolysis; transfer of milk serum; maintenance of emulsion into stability by prevention of globule fusion; availability of fatty acids and cholesterol for micellar absorption in the small intestine; and destabilization by creaming, clumping, churning, freeze-thaw, and heating, resulting in loosely bound substances into milk transfer serum. Worthy of notice is that the interactions are dynamic.Moreover, it is assumed that the MFGM proteins also possess specific nutritional properties. As such, due to their origin, composition and structure, MFGM polar lipids and proteins could be used as an emulsifier or stabilizer, combining technological and nutritional functionality [Mulder & Walstra, 1974;Anderson & Cawston, 1975;Patton & Keenan, 1975;Patton & Jensen, 1975, 1976Keenan et al., 1983;Mather & Keenan, 1983; McPherson & Kitchen, 1983; Walstra & Jenness, 1984;Keenan & Dylewski, 1985 Bucbheim, 1986;Mather, 1987; Keenan et al., 1988;Keenan & Dylewski, 1995;Keenan & Patton, 1995;Mather & Keenan, 1998;Danthine et al., 2000; Keenan, 2001; Keenan & Mather, 2002; Ollivier--Bousquet, 2002;Lopez et al., 2006Lopez et al., , 2007Sanchez-Juanes et al., 2009;Zamora et al., 2009]. Composition, Properties and Nutritional Aspects of Milk Fat Globule Membrane -a Review Mohamed Mansour El-Loly Dairy Department, National Research Centre, Dokki, Cairo, EgyptKey words: milk fat globule membrane, mammary gland, isolation, structure, stability, nutritional, nutraceuticalIn the last few years, knowledge on the composition and properties of the milk fat globule membrane (MFGM) increased significantly. It is now recognized that the MFGM is highly complex in structure and composed of different protein and lipid components with specific technological and nutritional properties. As such, MFGM materials have been isolated and characterized as valuable ingredients for incorporation into new food products. However, MFGM are also sensitive to modification during isolation and processing, and care should be taken to standardize the composition and characteristics of the membrane to maintain its unique properties during application in food products.The MFGM is subject to changes in composition and structure from the moment the fat globule leaves the mammary secretory cell. Upon milk harvesting and further milk handling, further changes to the MFGM take place. Depending on the type and degree of treatment, this may involve different physico-chemical interactions between various membrane components, the loss of membrane components and/or adsorption of components from the milk plasma. However, the effects appear to be variable and dependent on physiological (animal) factors, and much remains ...

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“…19 An optimal drug delivery system should be biocompatible, biodegradable and should not cause any immunological 19 Liposomes synthesized from dehydrated-rehydrated vesicles are widely used due to the ease of this preparation process and the low amount of stress applied to the proteins. 134 Liposome formulations are most frequently considered for parental administration of the drug, but may also be a potential formulation principle for alternative routes such as topical and nasal administration.…”

Section: Protein Encapsulationmentioning

confidence: 99%

Overview of the main methods used to combine proteins with nanosystems: absorption, bioconjugation, and encapsulation

Marco¹

2009

IJN

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Liposomes with phosphatidylethanol as a carrier for oral delivery of insulin: studies in the rat

Cited by 146 publications

References 29 publications

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

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

Composition, Properties and Nutritional Aspects of Milk Fat Globule Membrane – A Review

Overview of the main methods used to combine proteins with nanosystems: absorption, bioconjugation, and encapsulation

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