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Promising Applications in Drug Delivery Systems of a Novel β-cyclodextrin Derivative Obtained by Green Synthesis

Promising Applications in Drug Delivery Systems of a Novel β-cyclodextrin Derivative Obtained by Green Synthesis

Agustina García, Darío Leonardi, María C Lamas

Bioorg Med Chem Lett. 2016 Jan 15;26(2):602-608.

PMID: 26642766

Abstract:

An efficient and green method has been developed for the synthesis of succinyl-β-cyclodextrin in aqueous media obtaining very good yield. Acidic groups have been introduced in the synthesized carrier molecule to improve the guest-host affinity. To evaluate the suitability of the novel excipient focused to develop oral dosage forms, albendazole, a BSC class II compound, was chosen as a model drug. The β-cyclodextrin derivative and the inclusion complex were thoroughly characterized in solution and solid state by phase solubility studies, FT-IR spectroscopy, SEM, XRD, ESI-MS, DSC, 1D (1)H NMR, 1D (13)C NMR, selective 1D TOCSY, 2D COSY, 2D HSQC, 2D HMBC and ROESY NMR spectroscopy. Phase solubility studies indicated that both of them β-cyclodextrin and succinyl-β-cyclodextrin formed 1:1 inclusion complexes with albendazole, and the stability constants were 68M(-1) (β-cyclodextrin), 437M(-1) (succinyl-β-cyclodextrin), respectively. Water solubility and dissolution rate of albendazole were significantly improved in complex forms. Thus, the succinyl-β-cyclodextrin derivative could be a promising excipient to design oral dosage forms.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AR13113	Succinyl-β-cyclodextrin			Price

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