Protection of insulin from enzymatic degradation by its association to liposomes

Weingarten, Colette; Moufti, A.; Delattre, Jacques; Puisieux, F.; Couvreur, Patrick

doi:10.1016/0378-5173(85)90234-0

Cited by 31 publications

(8 citation statements)

References 12 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Composition of LiposomessDPPC/Ch (7/2)-MLV liposomes [12][13][14]16 and DPPC/Ch (7/7)-MLV liposomes 15 have been reported to be absorbed efficiently by oral administration of insulin liposomes. However, the 0.1-µm DPPC/Ch (7/4, 0.1)-Epo/liposomes ( Figure 5) were not absorbed.…”

Section: Discussionmentioning

confidence: 99%

“…Regarding liposome size, Aramaki et al reported that multilamellar liposomes (MLV) larger than 374 nm in size were taken up through rat Peyer's patches after oral administration using isolated tissues. 28 The MLV liposomes have been used in many cases for oral administration, [11][12][13][14][15] while REV liposomes have not.…”

Section: Discussionmentioning

confidence: 99%

“…[11][12][13][14][15] The use of liposomes as carriers of cytokines, 16 interleukin-2, 17 interleukin-7, 18 and interferon 19 has been reported, but that of Epo has not been studied in the past.…”

mentioning

confidence: 99%

See 2 more Smart Citations

Oral Administration of Recombinant Human Erythropoietin in Liposomes in Rats: Influence of Lipid Composition and Size of Liposomes on Bioavailability

Maitani

Hazama

Tojo

et al. 1996

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

Intestinal absorption of recombinant human erythropoietin (Epo) encapsulated in liposomes (Epo/liposomes) was examined by measuring the pharmacological effects of Epo after oral administration in rats. Circulating reticulocyte counts after oral administration of Epo/liposomes showed a profile different from that after intravenous administration. Epo/liposomes 0.1 micron in diameter were absorbed more effectively than those 0.2 micron in diameter. In the 0.1 micron Epo/liposomes composed of dipalmitoylphosphatidylcholine (DPPC) and soybean-derived sterols (SS), cholesterol (Ch), or soybean-derived sterylglucosides (SG), DPPC/SS (in molar ratio 7/2) and DPPC/Ch (7/2) showed higher efficiency in intestinal absorption than DPPC/Ch (7/4) and DPPC/SG (7/2) at a low dose by the sysmex method. Pharmacological availabilities for oral administration of Epo/liposomes were 0.74-31% and 3.3-30% as evaluated by circulating reticulocyte counts and percentage circulating reticulocytes of erythrocytes, respectively, in comparison to those for intravenous administration of the same dose.

show abstract

Section: Discussionmentioning

confidence: 99%

Section: Discussionmentioning

confidence: 99%

See 1 more Smart Citation

Oral Administration of Recombinant Human Erythropoietin in Liposomes in Rats: Influence of Lipid Composition and Size of Liposomes on Bioavailability

Maitani

Hazama

Tojo

et al. 1996

Journal of Pharmaceutical Sciences

View full text Add to dashboard Cite

show abstract

“…Results show that ionic interaction is involved in binding of insulin to phospholipids rather than hydrophobic association 119 . Accumulation of liposomes on the brush border membrane, enables absorption of insulin & the uptake of liposomes itself by peyer"s patches present in intestine also contribute to insulin absorption 120 .…”

Section: Fig 9: Plasma Levels Of Diabetic Rats After Oral Administratmentioning

confidence: 91%

Untitled

2013

IJPSR

View full text Add to dashboard Cite

The Present study focuses on the challenges facing the development of oral insulin the fact we have no formulation in market, being an attractive and advantageous over the regular injections. Physiological and biological factors of the insulin has great influence for the development of an oral formulation with many difficulties regarding the stability over gastric pH and proteolytic enzymes, selection of the proper formulation and its components depends on these conditions. The development with insulin therapy are needed with better patience compliance, low toxicity, higher glycemic control, thereby Diabetes related complications occurrence can be prevented. INTRODUCTION: In terms of efficacy, insulin in form of parental route is satisfactory, however it is associated with some severe adverse conditions like, peripheral hyperinsulinemia, smooth muscle cell proliferation, diabetic macro and micro angiopathy, lipoatrophy or lipohyertophy have become very common. Insulin delivery by oral route is not effective due to its susceptibility to enzymatic degradation in GI & Permeability across intestinal epithelium is low 1, 2. The proper combination of Multifunctional polymers will result a better biocompatible, biodegradable, hydrophilic and protective characteristic with better absorption orally in the GI 3 .

show abstract

“…Weingarten et al developed positively charged liposomes for insulin loading, and reported a protective action against insulin degradation in the presence of three digestive enzymes (pepsin, a-chymotrypsin and trypsin) [84]. As early as the 1970s, the use of liposomes for oral protein delivery was investigated using insulin as the model drug.…”

Section: Liposomes and Lipid Nanoparticlesmentioning

confidence: 99%