Drug release from starch-acetate microparticles and films with and without incorporated α-amylase

Laura Tuovinen (Corresponding Author), Soili Peltonen, Merja Liikola, Marika Hotakainen, M. Lahtela-Kakkonen, A. Poso, Kristiina Järvinen

Research output: Contribution to journalArticleScientificpeer-review

48 Citations (Scopus)

Abstract

Acetylation of starch considerably decreases its swelling and enzymatic degradation. Thus, starch-acetate (SA) based delivery systems may be suitable for controlled drug delivery. The aim of the present study was to evaluate drug release from the SA microparticles (SA mps) and SA films. The average degree of acetyl substitution (DS) per glucose residue in the starch was either 1.9 (SA DS 1.9) or 2.6 (SA DS 2.6). Timolol (mw 332), calcein (mw 623) and bovine serum albumin (BSA, mw 68,000) were used as model drugs. A continuous timolol release from the both SA mps was observed in phosphate buffer solution (PBS) pH 7.4 (50-days incubation). The release of timolol was faster from the SA DS 1.9 mps than from the SA DS 2.6 mps. Calcein release from both SA mps was continuous in PBS pH 7.4 (5-days incubation). But, calcein release profile from the SA DS 2.6 film in PBS pH 7.4 showed discontinuities. However, the release of calcein from both SA films was continuous in human serum in vitro during the 7-day incubation, i.e. enzymes enhanced calcein release. Thus, α-amylase was incorporated into the SA films in order to enhance drug release from the films. However, the effects of incorporation of α-amylase on the model macromolecule (BSA) release from the SA films were modest. In conclusion, this study demonstrates the achievement of slow release of different molecular weight model drugs from the SA mps and films as compared to fast release from the native starch preparations. DS of SA, physicochemical properties of a drug and the presence of enzymes can all affect drug release profiles from SA based preparations.
Original languageEnglish
Pages (from-to)4355 - 4362
Number of pages8
JournalBiomaterials
Volume25
Issue number18
DOIs
Publication statusPublished - 2004
MoE publication typeA1 Journal article-refereed

Fingerprint

Amylases
Starch
Pharmaceutical Preparations
Substitution reactions
Timolol
Buffers
Phosphates
starch acetate
Drug Liberation
Controlled drug delivery
Enzymes
Acetylation
Molecular Models
Bovine Serum Albumin
Macromolecules

Keywords

  • biopolymers

Cite this

Tuovinen, L., Peltonen, S., Liikola, M., Hotakainen, M., Lahtela-Kakkonen, M., Poso, A., & Järvinen, K. (2004). Drug release from starch-acetate microparticles and films with and without incorporated α-amylase. Biomaterials, 25(18), 4355 - 4362. https://doi.org/10.1016/j.biomaterials.2003.11.026
Tuovinen, Laura ; Peltonen, Soili ; Liikola, Merja ; Hotakainen, Marika ; Lahtela-Kakkonen, M. ; Poso, A. ; Järvinen, Kristiina. / Drug release from starch-acetate microparticles and films with and without incorporated α-amylase. In: Biomaterials. 2004 ; Vol. 25, No. 18. pp. 4355 - 4362.
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abstract = "Acetylation of starch considerably decreases its swelling and enzymatic degradation. Thus, starch-acetate (SA) based delivery systems may be suitable for controlled drug delivery. The aim of the present study was to evaluate drug release from the SA microparticles (SA mps) and SA films. The average degree of acetyl substitution (DS) per glucose residue in the starch was either 1.9 (SA DS 1.9) or 2.6 (SA DS 2.6). Timolol (mw 332), calcein (mw 623) and bovine serum albumin (BSA, mw 68,000) were used as model drugs. A continuous timolol release from the both SA mps was observed in phosphate buffer solution (PBS) pH 7.4 (50-days incubation). The release of timolol was faster from the SA DS 1.9 mps than from the SA DS 2.6 mps. Calcein release from both SA mps was continuous in PBS pH 7.4 (5-days incubation). But, calcein release profile from the SA DS 2.6 film in PBS pH 7.4 showed discontinuities. However, the release of calcein from both SA films was continuous in human serum in vitro during the 7-day incubation, i.e. enzymes enhanced calcein release. Thus, α-amylase was incorporated into the SA films in order to enhance drug release from the films. However, the effects of incorporation of α-amylase on the model macromolecule (BSA) release from the SA films were modest. In conclusion, this study demonstrates the achievement of slow release of different molecular weight model drugs from the SA mps and films as compared to fast release from the native starch preparations. DS of SA, physicochemical properties of a drug and the presence of enzymes can all affect drug release profiles from SA based preparations.",
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Tuovinen, L, Peltonen, S, Liikola, M, Hotakainen, M, Lahtela-Kakkonen, M, Poso, A & Järvinen, K 2004, 'Drug release from starch-acetate microparticles and films with and without incorporated α-amylase', Biomaterials, vol. 25, no. 18, pp. 4355 - 4362. https://doi.org/10.1016/j.biomaterials.2003.11.026

Drug release from starch-acetate microparticles and films with and without incorporated α-amylase. / Tuovinen, Laura (Corresponding Author); Peltonen, Soili; Liikola, Merja; Hotakainen, Marika; Lahtela-Kakkonen, M.; Poso, A.; Järvinen, Kristiina.

In: Biomaterials, Vol. 25, No. 18, 2004, p. 4355 - 4362.

Research output: Contribution to journalArticleScientificpeer-review

TY - JOUR

T1 - Drug release from starch-acetate microparticles and films with and without incorporated α-amylase

AU - Tuovinen, Laura

AU - Peltonen, Soili

AU - Liikola, Merja

AU - Hotakainen, Marika

AU - Lahtela-Kakkonen, M.

AU - Poso, A.

AU - Järvinen, Kristiina

PY - 2004

Y1 - 2004

N2 - Acetylation of starch considerably decreases its swelling and enzymatic degradation. Thus, starch-acetate (SA) based delivery systems may be suitable for controlled drug delivery. The aim of the present study was to evaluate drug release from the SA microparticles (SA mps) and SA films. The average degree of acetyl substitution (DS) per glucose residue in the starch was either 1.9 (SA DS 1.9) or 2.6 (SA DS 2.6). Timolol (mw 332), calcein (mw 623) and bovine serum albumin (BSA, mw 68,000) were used as model drugs. A continuous timolol release from the both SA mps was observed in phosphate buffer solution (PBS) pH 7.4 (50-days incubation). The release of timolol was faster from the SA DS 1.9 mps than from the SA DS 2.6 mps. Calcein release from both SA mps was continuous in PBS pH 7.4 (5-days incubation). But, calcein release profile from the SA DS 2.6 film in PBS pH 7.4 showed discontinuities. However, the release of calcein from both SA films was continuous in human serum in vitro during the 7-day incubation, i.e. enzymes enhanced calcein release. Thus, α-amylase was incorporated into the SA films in order to enhance drug release from the films. However, the effects of incorporation of α-amylase on the model macromolecule (BSA) release from the SA films were modest. In conclusion, this study demonstrates the achievement of slow release of different molecular weight model drugs from the SA mps and films as compared to fast release from the native starch preparations. DS of SA, physicochemical properties of a drug and the presence of enzymes can all affect drug release profiles from SA based preparations.

AB - Acetylation of starch considerably decreases its swelling and enzymatic degradation. Thus, starch-acetate (SA) based delivery systems may be suitable for controlled drug delivery. The aim of the present study was to evaluate drug release from the SA microparticles (SA mps) and SA films. The average degree of acetyl substitution (DS) per glucose residue in the starch was either 1.9 (SA DS 1.9) or 2.6 (SA DS 2.6). Timolol (mw 332), calcein (mw 623) and bovine serum albumin (BSA, mw 68,000) were used as model drugs. A continuous timolol release from the both SA mps was observed in phosphate buffer solution (PBS) pH 7.4 (50-days incubation). The release of timolol was faster from the SA DS 1.9 mps than from the SA DS 2.6 mps. Calcein release from both SA mps was continuous in PBS pH 7.4 (5-days incubation). But, calcein release profile from the SA DS 2.6 film in PBS pH 7.4 showed discontinuities. However, the release of calcein from both SA films was continuous in human serum in vitro during the 7-day incubation, i.e. enzymes enhanced calcein release. Thus, α-amylase was incorporated into the SA films in order to enhance drug release from the films. However, the effects of incorporation of α-amylase on the model macromolecule (BSA) release from the SA films were modest. In conclusion, this study demonstrates the achievement of slow release of different molecular weight model drugs from the SA mps and films as compared to fast release from the native starch preparations. DS of SA, physicochemical properties of a drug and the presence of enzymes can all affect drug release profiles from SA based preparations.

KW - biopolymers

U2 - 10.1016/j.biomaterials.2003.11.026

DO - 10.1016/j.biomaterials.2003.11.026

M3 - Article

VL - 25

SP - 4355

EP - 4362

JO - Biomaterials

JF - Biomaterials

SN - 0142-9612

IS - 18

ER -

Tuovinen L, Peltonen S, Liikola M, Hotakainen M, Lahtela-Kakkonen M, Poso A et al. Drug release from starch-acetate microparticles and films with and without incorporated α-amylase. Biomaterials. 2004;25(18):4355 - 4362. https://doi.org/10.1016/j.biomaterials.2003.11.026