Materials and structure of polysaccharide-based delivery carriers for oral insulin: A review

Wang, Xinran; Sun, Hongnan; Mu, Taihua

doi:10.1016/j.carbpol.2023.121364

Cited by 4 publications

(1 citation statement)

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“…In the presence of divalent cations, such as calcium, sodium alginate crosslinks and forms a polymer matrix that controls drug release at specific pH [ 21 ]. Lower pH inhibits the release of drugs, as sodium alginate microparticles are stable in acidic conditions, while higher pH promotes the disintegration of the microsphere structure, thus increasing release rate [ 22 ]. The formulation of insulin-loaded calcium cross-linked sodium-alginate microparticles containing different non-ionic surfactants has not been particularly investigated.…”

Section: Introductionmentioning

confidence: 99%

Formulation and Evaluation of Insulin-Loaded Sodium-Alginate Microparticles for Oral Administration

Bácskay,

Papp,

Pártos

et al. 2023

Pharmaceutics

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The development of oral insulin drug delivery systems is still an ongoing challenge for pharmaceutical technology researchers, as the formulation process has to overcome a number of obstacles due to the adverse characteristics of peptides. The aim of this study was to formulate different sodium-alginate microparticles as a possible method for oral insulin administration. In our previous studies, the method has been successfully optimized using a small model peptide. The incorporation of insulin into alginate carriers containing nonionic surfactants has not been described yet. In order to enhance the absorption of insulin through biological barriers, Labrasol ALF and Labrafil M 2125 CS were selected as permeation-enhancing excipients. They were applied at a concentration of 0.10% (v/v%), along with various combinations of the two, to increase oral bioavailability. Encapsulation efficiency showed sufficient drug incorporation, as it resulted in over 80% in each composition. In vitro dissolution and enzymatic stability test results proved that, as a pH-responsive polymer, alginate bead swelling and drug release occur at higher pH, thus protecting insulin against the harsh environment of the gastrointestinal tract. The remaining insulin content was 66% due to SIF degradation after 120 min. Permeability experiments revealed the impact of permeation enhancers and natural polymers on drug absorption, as they enhanced drug transport significantly through Caco-2 cells in the case of alginate microparticle formulations, as opposed to the control insulin solution. These results suggest that these formulations are able to improve the oral bioavailability of insulin.

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Section: Introductionmentioning

confidence: 99%