首页|Encapsulation and release of As pidasept peptides in polysaccharide formulation for oral application

Encapsulation and release of As pidasept peptides in polysaccharide formulation for oral application

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  • NSTL
  • Elsevier
Due to the increase in bacterial resistance to common antibiotics and the lack of newly approved drugs, antimicrobial peptides (AMP) have been shown to be an alternative to combat infections caused by drug-resistant organisms. In particular, synthetic anti-lipopolysaccharide peptides (SALP) with the lead structure Aspidasept (Pep19-2.5) display a high anti-inflammatory activity in vitro and in vivo systems of endotoxemia and bacteremia. This was found not only when SALP were applied systemically (i.e. against sepsis), but also in topical therapies aimed at treating wound infections. A further important application involves combating common pathologies of the gastrointestinal tract, such as chronic infections of the small intestine and the colon (e.g., Crohn's disease). For the necessary oral application, the active pharmaceutical ingredient (API), Aspidasept (R), must be encapsulated to ensure its protection against the low pH and the hydrolytic enzymes of the gastrointestinal tract. Here, the encapsulation of Aspidasept in polysaccharide matrices, essentially alginate and pectin, was systematically investigated with a variety of physico-chemical techniques. Specifically, we characterized key features of the nanoparticles such as their sizes and size distributions, as well as their stability in different environments mimicking digestive fluids. Finally, we studied the release of the drug from the polysaccharide matrices and the ability of nanoparticles to neutralize endotoxemia in vitro. We showed that our lead formulations exert an optimum inhibitory activity on immune cells stimulated by lipopolysaccharide.

Antimicrobial peptidesDrug encapsulationLipopolysaccharidePolysaccharide matricesChronical intestine inflammation

Kuhlmann, Nicole、Nehls, Christian、Heinbockel, Lena、Correa, Wilmar、Moll, Ralf、Gutsmann, Thomas、Huebner, Christian、Englisch, Uwe、Brandenburg, Klaus

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Tech Hsch Lubeck, Monkhofer Weg 239, D-23562 Lubeck, Germany

Leibniz Lungenzentrum, Forschungszentrum Borstel, Parkallee, D-23845 Borstel, Germany

Univ Lubeck, Inst Phys, Ratzeburger Allee 160, D-23562 Lubeck, Germany

Brandenburg Antiinfekt GmbH, Forschungszentrum Borstel, Parkallee 10b, D-23845 Borstel, Germany

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2021

10.1016/j.ejps.2020.105687

European journal of pharmaceutical sciences

European journal of pharmaceutical sciences

ISTP
ISSN：0928-0987
年,卷(期)：2021.158
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