Preformulation Studies and Bioavailability Enhancement of Curcumin with a 'Two in One' PEG-β-Cyclodextrin Polymer

被引：3

作者：

Haimhoffer, Adam ^{[1
,2
,3
]}

Dossi, Eleftheria ^{[4
]}

Beresova, Monika ^{[5
]}

Bacskay, Ildiko ^{[1
,3
]}

Varadi, Judit ^{[1
]}

Afsar, Ashfaq ^{[4
]}

Rusznyak, Agnes ^{[1
]}

Vasvari, Gabor ^{[1
]}

Fenyvesi, Ferenc ^{[1
]}

机构：

[1] Univ Debrecen, Fac Pharm, Dept Pharmaceut Technol, Nagyerdei St 98, H-4032 Debrecen, Hungary

[2] Univ Debrecen, Doctoral Sch Pharmaceut Sci, H-4032 Debrecen, Hungary

[3] Univ Debrecen, Inst Healthcare Ind, Nagyerdei St 98, H-4032 Debrecen, Hungary

[4] Cranfield Univ, Cranfield Def & Secur, Swindon SN6 8LA, Wilts, England

[5] Univ Debrecen, Dept Med Imaging, Nagyerdei Krt 94, H-4032 Debrecen, Hungary

来源：

PHARMACEUTICS | 2021年 / 13卷 / 10期

关键词：

curcumin; PEG-cyclodextrin polymer; complexation; bioavailability; NMR; WATER-SOLUBLE POLYMERS; INCLUSION COMPLEX; SOLUBILITY; HYDROGELS; TECHNOLOGY; RELEASE; CHAINS;

D O I：

10.3390/pharmaceutics13101710

中图分类号：

R9 [药学];

学科分类号：

1007 ;

摘要：

Drug delivery systems are used to improve the biopharmaceutical properties of curcumin. Our aim was to investigate the effect of a water-soluble 'two in one' polymer containing covalently bonded PEG and beta CD moieties (beta CPCD) on the solubility and bioavailability of curcumin and compare it to a polymeric beta-cyclodextrin (beta CDP) cross-linked with epichlorohydrin. Phase-solubility and dynamic light scattering (DLS) experiments showed that the solubility of curcumin increased significantly in 10 m/m % beta CPCD and beta CDP solutions, but beta CPCD-curcumin particles had higher hydrodynamic volume. The formation of the beta CPCD-curcumin complex in solution and sedimented phase was confirmed by NMR spectroscopy. Biocompatibility and permeability experiments were performed on Caco-2 cells. Polymers did not show cytotoxicity up to 10 m/m % and beta CPCD significantly increased the permeability of curcumin. DLS measurements revealed that among the interaction of polymers with mucin, beta CPCD formed bigger aggregates compared to beta CDP. Curcumin complexes were lyophilized into capsules and structurally characterized by micro-CT spectroscopy. Drug release was tested in a pH 1.2 medium. Lyophilized complexes had a solid porous matrix and both beta CPCD and beta CDP showed rapid drug release. beta CPCD provides an opportunity to create a swellable, mucoadhesive matrix system for oral drug delivery.</p>

引用

页数：17

共 43 条

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