Poly(curcumin β-amino ester)-Based Tablet Formulation for a Sustained Release of Curcumin

Vinod S. Patil; Benjamin C. Burdette; J. Zach Hilt; Douglass S. Kalika; Thomas D. Dziubla

doi:10.3390/gels8060337

Poly(curcumin β-amino ester)-Based Tablet Formulation for a Sustained Release of Curcumin

Vinod S. Patil, Benjamin C. Burdette, J. Zach Hilt, Douglass S. Kalika, Thomas D. Dziubla

Research output: Contribution to journal › Article › peer-review

2 Scopus citations

Abstract

Oral drug delivery remains the most common and well tolerated method for drug admin-istration. However, its applicability is often limited due to low drug solubility and stability. One approach to overcome the solubility and stability limitations is the use of amorphous polymeric pro-drug formulations, such as poly(β-amino ester) (PBAE). PBAE hydrogels, which are biodegradable and pH responsive, have shown promising results for the controlled release of drugs by improving the stability and increasing the solubility of these drugs. In this work, we have evaluated the potential use of PBAE prodrugs in an oral tablet formulation, studying their sustained drug release potential and storage stability. Curcumin, a low solubility, low stability antioxidant drug was used as a model compound. Poly(curcumin β-amino ester) (PCBAE), a crosslinked amorphous network, was synthesized by a previously published method using a commercial diacrylate and a primary diamine, in combination with acrylate-functionalized curcumin. PCBAE-based tablets were made and exhibited a sustained release for 16 h, following the hydrolytic degradation of PCBAE particles into native curcumin. In addition to the release studies, preliminary storage stability was assessed using standard and accelerated stability conditions. As PCBAE degradation is hydrolysis driven, tablet stability was found to be sensitive to moisture.

Original language	English
Article number	337
Journal	Gels
Volume	8
Issue number	6
DOIs	https://doi.org/10.3390/gels8060337
State	Published - Jun 2022

Bibliographical note

Funding Information:
Funding: The project described was supported by the NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879 and industrial contributions). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Science Foundation.

Funding Information:
The project described was supported by the NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879 and industrial contributions). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Science Foundation.

Publisher Copyright:
© 2022 by the authors. Licensee MDPI, Basel, Switzerland.

Keywords

Poy(β-amino ester)
amorphous
controlled drug delivery
crosslinked systems
curcumin
hydrogels
oral dosage form
prodrug
solubility
tablets

ASJC Scopus subject areas

Bioengineering
Biomaterials
Organic Chemistry
Polymers and Plastics

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10.3390/gels8060337

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title = "Poly(curcumin β-amino ester)-Based Tablet Formulation for a Sustained Release of Curcumin",

abstract = "Oral drug delivery remains the most common and well tolerated method for drug admin-istration. However, its applicability is often limited due to low drug solubility and stability. One approach to overcome the solubility and stability limitations is the use of amorphous polymeric pro-drug formulations, such as poly(β-amino ester) (PBAE). PBAE hydrogels, which are biodegradable and pH responsive, have shown promising results for the controlled release of drugs by improving the stability and increasing the solubility of these drugs. In this work, we have evaluated the potential use of PBAE prodrugs in an oral tablet formulation, studying their sustained drug release potential and storage stability. Curcumin, a low solubility, low stability antioxidant drug was used as a model compound. Poly(curcumin β-amino ester) (PCBAE), a crosslinked amorphous network, was synthesized by a previously published method using a commercial diacrylate and a primary diamine, in combination with acrylate-functionalized curcumin. PCBAE-based tablets were made and exhibited a sustained release for 16 h, following the hydrolytic degradation of PCBAE particles into native curcumin. In addition to the release studies, preliminary storage stability was assessed using standard and accelerated stability conditions. As PCBAE degradation is hydrolysis driven, tablet stability was found to be sensitive to moisture.",

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note = "Funding Information: Funding: The project described was supported by the NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879 and industrial contributions). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Science Foundation. Funding Information: The project described was supported by the NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879 and industrial contributions). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Science Foundation. Publisher Copyright: {\textcopyright} 2022 by the authors. Licensee MDPI, Basel, Switzerland.",

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AU - Dziubla, Thomas D.

N1 - Funding Information: Funding: The project described was supported by the NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879 and industrial contributions). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Science Foundation. Funding Information: The project described was supported by the NSF I/UCRC Center for Pharmaceutical Development (IIP-1063879 and industrial contributions). The content is solely the responsibility of the authors and does not necessarily represent the official views of the National Science Foundation. Publisher Copyright: © 2022 by the authors. Licensee MDPI, Basel, Switzerland.

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N2 - Oral drug delivery remains the most common and well tolerated method for drug admin-istration. However, its applicability is often limited due to low drug solubility and stability. One approach to overcome the solubility and stability limitations is the use of amorphous polymeric pro-drug formulations, such as poly(β-amino ester) (PBAE). PBAE hydrogels, which are biodegradable and pH responsive, have shown promising results for the controlled release of drugs by improving the stability and increasing the solubility of these drugs. In this work, we have evaluated the potential use of PBAE prodrugs in an oral tablet formulation, studying their sustained drug release potential and storage stability. Curcumin, a low solubility, low stability antioxidant drug was used as a model compound. Poly(curcumin β-amino ester) (PCBAE), a crosslinked amorphous network, was synthesized by a previously published method using a commercial diacrylate and a primary diamine, in combination with acrylate-functionalized curcumin. PCBAE-based tablets were made and exhibited a sustained release for 16 h, following the hydrolytic degradation of PCBAE particles into native curcumin. In addition to the release studies, preliminary storage stability was assessed using standard and accelerated stability conditions. As PCBAE degradation is hydrolysis driven, tablet stability was found to be sensitive to moisture.

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Poly(curcumin β-amino ester)-Based Tablet Formulation for a Sustained Release of Curcumin

Abstract

Bibliographical note

Keywords

ASJC Scopus subject areas

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