In vitro and in vivo evaluation ofanovel self-assembled oral delivery system for hydrophobic drugs

Objective To design and synthesize a new hydrophilic aspartic acid peptide derivative, poly(isopropyl-D, L-aspartamide) (PIPAA), and investigate its efficiency to self-assemble with carboxy-containing therapeutics into pH-sensitive microspheres to enhance the dissolution and oral bioavailability of...

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Bibliographic Details
Published inDi 3 jun yi da xue xue bao Vol. 42; no. 10; pp. 1053 - 1058
Main Authors ZHAO Yang, LIU Renfeng, DOU Yin, GUO Jiawei, ZHANG Jianxiang
Format Journal Article
LanguageChinese
Published Editorial Office of Journal of Third Military Medical University 01.05.2020
Subjects
insoluble drugs
intestinal targeting
l-aspartamide
ph-sensitivity
poly(isopropyl-d
self-assembly
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Summary:Objective To design and synthesize a new hydrophilic aspartic acid peptide derivative, poly(isopropyl-D, L-aspartamide) (PIPAA), and investigate its efficiency to self-assemble with carboxy-containing therapeutics into pH-sensitive microspheres to enhance the dissolution and oral bioavailability of hydrophobic drugs. Methods With phosphoric acid as the catalyst, D, L-aspartic acid was polymerized into polysuccinimide (PSI) at 180 ℃ followed by ring-opening reaction with isopropylamine to form PIPAA. The successful synthesis of PSI and PIPAA was characterized by Fourier transform infrared spectroscopy (FT-IR) and 1H NMR spectroscopy. The morphology, size, drug loading content and loading efficiency of IND/PIPAA microspheres were characterized. FT-IR and 1H NMR spectroscopy were used to determine non-covalent forces between IND and PIPAA in IND/PIPAA microspheres, and the existence form of IND in IND/PIPAA microspheres was examined by differential scanning calorimetry (DSC) and Xray diffraction (XRD) measuremen
ISSN:1000-5404
DOI:10.16016/j.1000-5404.202001169