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Formulation and Optimization of Zinc-Pectinate Beads for the Controlled Delivery of Resveratrol

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Abstract

Preventive and therapeutic efficacies of resveratrol on several lower gastrointestinal (GI) diseases (e.g., colorectal cancer, colitis) are well documented. To overcome the problems due to its rapid absorption and metabolism at the upper GI tract, a delayed release formulation of resveratrol was designed to treat these lower GI diseases. The current study aimed to develop a delayed release formulation of resveratrol as multiparticulate pectinate beads by varying different formulation parameters. Zinc-pectinate (Zn-pectinate) beads exhibited better delayed drug release pattern than calcium-pectinate (Ca-pectinate) beads. The effects of the formulation parameters were investigated on shape, size, Zn content, moisture content, drug encapsulation efficiency, swelling–erosion, and resveratrol retention pattern of the formulated beads. Upon optimization of the formulation parameters in relative to the drug release profiles, the optimized beads were further subjected to morphological, chemical interaction, enzymatic degradation, and stability studies. Almost all prepared beads were spherical with ∼1 mm diameter and efficiently encapsulated resveratrol. The formulation parameters revealed great influence on resveratrol retention and swelling–erosion behavior. In most of the cases, the drug release data more appropriately fitted with zero-order equation. This study demonstrates that the optimized Zn-pectinate beads can encapsulate very high amount of resveratrol and can be used as delayed release formulation of resveratrol.

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Abbreviations

Ca:

calcium

CaCl2 :

calcium chloride

Ca-pectinate:

calcium-pectinate

Ca2+ :

calcium cation

EE:

encapsulation efficiency

ER:

elongation ratio

FD:

freeze drying

FTIR:

Fourier transform infra-red

GI tract:

gastrointestinal tract

MC:

moisture content

P–R:

pectin–resveratrol

RT:

room temperature

SER:

swelling–erosion ratio

T 25 :

25% drug retention

T 50 :

50% drug retention

T 75 :

75% drug retention

Zn(CH3COO)2 :

zinc acetate

Zn:

zinc

Zn-pectinate:

zinc-pectinate

Zn2+ :

zinc cation

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Acknowledgments

This work was partially supported through a National University of Singapore Academic Research Funds R148-050-068-101 and R148-050-068-133.

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Author notes

  1. Ka-Yun Ng

    Present address: National Institutes of Health, Bethesda,, Maryland, 20892, USA

Authors and Affiliations

  1. Department of Pharmacy, Faculty of Science, National University of Singapore, Block S4, 18 Science Drive 4, Singapore, 117543, Republic of Singapore

    Surajit Das, Ka-Yun Ng & Paul C. Ho

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Das, S., Ng, KY. & Ho, P.C. Formulation and Optimization of Zinc-Pectinate Beads for the Controlled Delivery of Resveratrol. AAPS PharmSciTech 11, 729–742 (2010). https://doi.org/10.1208/s12249-010-9435-7

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  • DOI: https://doi.org/10.1208/s12249-010-9435-7

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