Chitosan for enhanced intestinal permeability: Prospects for derivatives soluble in neutral and basic environments

Kotzé, A.F; Lueßen, H.L.; Boer, A.G. de; Verhoef, J.; Junginger, Hans E.

doi:10.1016/s0928-0987(98)00016-5

Cited by 175 publications

(82 citation statements)

References 24 publications

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“…Chitosan, being a weak base, loses its charge with subsequent precipitation in neutral and basic environment thus proving to be ineffective as an absorption enhancer, limiting its use in the alkaline pH of the intestine and colon. A similar phenomenon was demonstrated by Kotze et al (1998a). No significant increase in the transport of 14 C mannitol at pH 7.4 in the presence of chitosan salts (glutamate and hydrochloride ; both degree of deacetylation 83 %) was observed.…”

Section: Controlled Drug Deliverysupporting

confidence: 81%

Chitosan: some pharmaceutical and biological aspects - an update

Singla

Chawla

2001

Journal of Pharmacy and Pharmacology

704

363

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Chitosan, a natural polysaccharide, is being widely used as a pharmaceutical excipient. It is obtained by the partial deacetylation of chitin, the second most abundant natural polymer.Chitosan comprises a series of polymers varying in their degree of deacetylation, molecular weight, viscosity, pKa etc. The presence of a number of amino groups permit chitosan to chemically react with anionic systems, thereby resulting in alteration of physicochemical characteristics of such combinations.Chitosan has found wide applicability in conventional pharmaceutical devices as a potential formulation excipient, some of which include binding, disintegrating and tablet coating properties. The polymer has also been investigated as a potential adjuvant for swellable controlled drug delivery systems. Use of chitosan in novel drug delivery as mucoadhesive, gene and peptide drug administration via the oral route as well as its absorption enhancing effects have been explored by a number of researchers.Chitosan exhibits myriad biological actions, namely hypocholesterolemic, antimicrobial and wound healing properties. Low toxicity coupled with wide applicability makes it a promising candidate not only for the purpose of drug delivery for a host of drug moieties (antiinflammatories, peptides etc.) but also as a biologically active agent.It is the endeavour of the present review to provide an insight into the biological and pharmaceutical profile of chitosan. Various investigations carried out recently are reported, although references to research performed on chitosan prior to the recent reviews have also been included, where appropriate.

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Section: Controlled Drug Deliverysupporting

confidence: 81%

Chitosan: some pharmaceutical and biological aspects - an update

Singla

Chawla

2001

Journal of Pharmacy and Pharmacology

704

363

View full text Add to dashboard Cite

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“…Recent studies have shown that only protonated, soluble chitosan can trigger the opening of tight junctions and thereby facilitate the paracellular transport of hydrophilic mannitol 52 . To improve the poor water solubility of chitosan, some derivatives were synthesized, such as polyethylene glycol (PEG)-chitosan 53 and trimethyl chitosan 54,55 .…”

Section: Mucoadhesive Polymers Used In Nasal Drug Deliverymentioning

confidence: 99%

Untitled

2017

IJPSR

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Nasal drug delivery has been recognized as a promising route for delivery of therapeutic compounds including biopharmaceuticals. It has been demonstrated that absorption of drugs can enhanced by using absorption enhancers or increasing the drug residence time in the nasal cavity. Mucoadhesive polymers can serve both functions. The residence time in the nasal cavity is considerably increased for microspheres compared to solutions. However, this is not the only factor to increase the absorption of large hydrophilic drugs. Microspheres also exert a direct effect on the mucosa, resulting in the opening of tight junctions between the epithelial cells. This review focuses on the background of nasal mucoadhesive drug delivery with special references to the biological and pharmaceutical considerations for nasal mucoadhesive drug administration.

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“…Polymeric delivery systems, including chitosan and its derivatives, have mucoadhesive properties, good water solubility and tight junction modulatory effects. N-trimethyl chitosan chloride (TMC) is a well described and studied cationic polymer that opens tight junctions and improves paracellular diffusion of hydrophilic drug molecules [16,17]. The absorption enhancing effect of TMC can be attributed to interactions of the fixed positively charged quaternary amino groups on the C-2 position of TMC directly and indirectly with the cell membranes [18,19].…”

Section: ________________________________________mentioning

confidence: 99%

Nasal Delivery of Recombinant Human Growth Hormone: In Vivo Evaluation with Pheroid™ Technology and N-Trimethyl Chitosan Chloride

Steyn¹,

Plessis

Kotzé³

2010

J Pharm Pharm Sci

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-Purpose. It was the aim of this study to investigate the possible enhancement of the absorption of recombinant human growth hormone (rhGH) in the nasal cavity, in the presence of a polymeric absorption enhancer, N-trimethyl chitosan chloride (TMC) and a patented fatty acid-based delivery system, Pheroid. Methods. Two types of Pheroid formulations, Pheroid vesicles and Pheroid microsponges were characterized and evaluated with regard to particle size and morphology. In vivo bioavailability studies in rats were performed and the nasal bioavailability of Pheroid vesicles and Pheroid microsponges were compared relative to subcutaneous administration. The results were also compared with different N-trimethyl chitosan chloride (TMC) formulations, TMC H-L and TMC H-H, well studied absorption enhancers. Results. Pheroid vesicles and Pheroid microsponges showed a size distribution of approximately 2-3 µm and 3-4 µm for Pheroid vesicles and Pheroid microsponges respectively. Using specific RIA, the relative bioavailability of rhGH after comparison with subcutaneous injection was determined to be 38.9, 128.5, 39.9, 136.3, and 8.3 % for Pheroid microsponges, Pheroid vesicles, TMC H-H, TMC H-L and control group (intranasal rhGH alone), respectively. All the enhancers showed significant absorption enhancement (P < 0.05) with the highest effect observed with TMC H-L. Conclusion. All the enhancers may have promising potential as safe and effective nasal absorption enhancers of rhGH.The Pheroid delivery system is a novel patented system consisting of a unique submicron emulsion type formulation. The system, which consist mainly of essential fatty acids can entrap and transport pharmacological active compounds. In this study it is shown that two types of Pheroid formulations, Pheroid vesicles and Pheroid microsponges, have the ability to entrap recombinant human growth hormone and improve the nasal absorption and thus bioavailability of rhGH. Intranasal administration of rhGH entrapped in Pheroid technology is an attractive alternative to subcutaneous of intravenous administration. _______________________________________________________________________________________

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Chitosan for enhanced intestinal permeability: Prospects for derivatives soluble in neutral and basic environments

Cited by 175 publications

References 24 publications

Chitosan: some pharmaceutical and biological aspects - an update

Chitosan: some pharmaceutical and biological aspects - an update

Untitled

Nasal Delivery of Recombinant Human Growth Hormone: In Vivo Evaluation with Pheroid™ Technology and N-Trimethyl Chitosan Chloride

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