Formulation Design and <i>in vitro-in vivo</i> Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids

Chekwube Andrew Ezegbe; Salome Amarachi Chime; Lydia Onyinyechi Ugorji; Calister Elochukwu Ugwu; Amarachi Kalu Agu; Oluebube Chisom Onyia; Godswill Onunkwo

doi:doi:10.11648/j.ajbes.20210704.14

Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids

Chekwube Andrew Ezegbe, Salome Amarachi Chime, Lydia Onyinyechi Ugorji, Calister Elochukwu Ugwu, Amarachi Kalu Agu, Oluebube Chisom Onyia, Godswill Onunkwo

Published in American Journal of Biological and Environmental Statistics (Volume 7, Issue 4)

Received: 10 November 2021 Accepted: 27 November 2021 Published: 2 December 2021

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Abstract

Background: PEGylation is a strategy that on therapeutic molecules such as drugs, proteins and macromolecules, in order to improve their delivery. It has this unique property of increasing the size and molecular weight of biomolecules that are conjugated in nature in order to improve water solubility, reduction in renal clearance and protects the drug from enzymatic degradation. Objectives: The objectives of this work was to formulate sustained release aspirin-loaded solid lipid microparticles based on PEGylated lipid matrix, to evaluate the in-vitro properties of the SLM and to study the anti-inflammatory and ulcerogenic properties of the SLM. Methods: Aspirin-loaded solid lipid microparticles (SLMs) were formulated by cold homogenization method. Furthermore, they were analyzed for the encapsulation efficiency, in-vitro release, particle size, anti-inflammatory and ulcer inhibition properties. Results: Particle size ranged from 9.36±2.63 to 16.77±5.80 µm for batches B₁ to D₁ SLMs loaded with 10% LM, 5% PEG 4000 and 0.25-1% aspirin respectively, while batches B₂ to D₂ formulated with 10% LM, 10% PEG and 0.25 -1% aspirin had particle size range of 9.09±4.03 to 15.71±10.09 µm. Batches D₁ containing 1% of aspirin had the highest encapsulation efficiency of 58%. Maximum in-vitro release of 29.20% and 15.85% were obtained at 6 h for batches D₁ and B₂ respectively. SLMs showed an average of 66.67 – 83.3% oedema inhibition, while the reference had 50%, and ulcer inhibition of 75% for batch D₁. Conclusion: Due to the good properties exhibited by the aspirin-loaded SLMS, they could be used for the treatment of inflammation.

Published in	American Journal of Biological and Environmental Statistics (Volume 7, Issue 4)
DOI	10.11648/j.ajbes.20210704.14
Page(s)	94-103
Creative Commons	This is an Open Access article, distributed under the terms of the Creative Commons Attribution 4.0 International License (http://creativecommons.org/licenses/by/4.0/), which permits unrestricted use, distribution and reproduction in any medium or format, provided the original work is properly cited.
Copyright	Copyright © The Author(s), 2021. Published by Science Publishing Group

Keywords

PEGylation, Solubility, Solid-lipid Microparticles, Aspirin, Cold Homogenization, Ulcer

References

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APA Style

Chekwube Andrew Ezegbe, Salome Amarachi Chime, Lydia Onyinyechi Ugorji, Calister Elochukwu Ugwu, Amarachi Kalu Agu, et al. (2021). Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids. American Journal of Biological and Environmental Statistics, 7(4), 94-103. https://doi.org/10.11648/j.ajbes.20210704.14

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ACS Style

Chekwube Andrew Ezegbe; Salome Amarachi Chime; Lydia Onyinyechi Ugorji; Calister Elochukwu Ugwu; Amarachi Kalu Agu, et al. Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids. Am. J. Biol. Environ. Stat. 2021, 7(4), 94-103. doi: 10.11648/j.ajbes.20210704.14

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AMA Style

Chekwube Andrew Ezegbe, Salome Amarachi Chime, Lydia Onyinyechi Ugorji, Calister Elochukwu Ugwu, Amarachi Kalu Agu, et al. Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids. Am J Biol Environ Stat. 2021;7(4):94-103. doi: 10.11648/j.ajbes.20210704.14

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@article{10.11648/j.ajbes.20210704.14,
  author = {Chekwube Andrew Ezegbe and Salome Amarachi Chime and Lydia Onyinyechi Ugorji and Calister Elochukwu Ugwu and Amarachi Kalu Agu and Oluebube Chisom Onyia and Godswill Onunkwo},
  title = {Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids},
  journal = {American Journal of Biological and Environmental Statistics},
  volume = {7},
  number = {4},
  pages = {94-103},
  doi = {10.11648/j.ajbes.20210704.14},
  url = {https://doi.org/10.11648/j.ajbes.20210704.14},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.ajbes.20210704.14},
  abstract = {Background: PEGylation is a strategy that on therapeutic molecules such as drugs, proteins and macromolecules, in order to improve their delivery. It has this unique property of increasing the size and molecular weight of biomolecules that are conjugated in nature in order to improve water solubility, reduction in renal clearance and protects the drug from enzymatic degradation. Objectives: The objectives of this work was to formulate sustained release aspirin-loaded solid lipid microparticles based on PEGylated lipid matrix, to evaluate the in-vitro properties of the SLM and to study the anti-inflammatory and ulcerogenic properties of the SLM. Methods: Aspirin-loaded solid lipid microparticles (SLMs) were formulated by cold homogenization method. Furthermore, they were analyzed for the encapsulation efficiency, in-vitro release, particle size, anti-inflammatory and ulcer inhibition properties. Results: Particle size ranged from 9.36±2.63 to 16.77±5.80 µm for batches B1 to D1 SLMs loaded with 10% LM, 5% PEG 4000 and 0.25-1% aspirin respectively, while batches B2 to D2 formulated with 10% LM, 10% PEG and 0.25 -1% aspirin had particle size range of 9.09±4.03 to 15.71±10.09 µm. Batches D1 containing 1% of aspirin had the highest encapsulation efficiency of 58%. Maximum in-vitro release of 29.20% and 15.85% were obtained at 6 h for batches D1 and B2 respectively. SLMs showed an average of 66.67 – 83.3% oedema inhibition, while the reference had 50%, and ulcer inhibition of 75% for batch D1. Conclusion: Due to the good properties exhibited by the aspirin-loaded SLMS, they could be used for the treatment of inflammation.},
 year = {2021}
}

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TY  - JOUR
T1  - Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids
AU  - Chekwube Andrew Ezegbe
AU  - Salome Amarachi Chime
AU  - Lydia Onyinyechi Ugorji
AU  - Calister Elochukwu Ugwu
AU  - Amarachi Kalu Agu
AU  - Oluebube Chisom Onyia
AU  - Godswill Onunkwo
Y1  - 2021/12/02
PY  - 2021
N1  - https://doi.org/10.11648/j.ajbes.20210704.14
DO  - 10.11648/j.ajbes.20210704.14
T2  - American Journal of Biological and Environmental Statistics
JF  - American Journal of Biological and Environmental Statistics
JO  - American Journal of Biological and Environmental Statistics
SP  - 94
EP  - 103
PB  - Science Publishing Group
SN  - 2471-979X
UR  - https://doi.org/10.11648/j.ajbes.20210704.14
AB  - Background: PEGylation is a strategy that on therapeutic molecules such as drugs, proteins and macromolecules, in order to improve their delivery. It has this unique property of increasing the size and molecular weight of biomolecules that are conjugated in nature in order to improve water solubility, reduction in renal clearance and protects the drug from enzymatic degradation. Objectives: The objectives of this work was to formulate sustained release aspirin-loaded solid lipid microparticles based on PEGylated lipid matrix, to evaluate the in-vitro properties of the SLM and to study the anti-inflammatory and ulcerogenic properties of the SLM. Methods: Aspirin-loaded solid lipid microparticles (SLMs) were formulated by cold homogenization method. Furthermore, they were analyzed for the encapsulation efficiency, in-vitro release, particle size, anti-inflammatory and ulcer inhibition properties. Results: Particle size ranged from 9.36±2.63 to 16.77±5.80 µm for batches B1 to D1 SLMs loaded with 10% LM, 5% PEG 4000 and 0.25-1% aspirin respectively, while batches B2 to D2 formulated with 10% LM, 10% PEG and 0.25 -1% aspirin had particle size range of 9.09±4.03 to 15.71±10.09 µm. Batches D1 containing 1% of aspirin had the highest encapsulation efficiency of 58%. Maximum in-vitro release of 29.20% and 15.85% were obtained at 6 h for batches D1 and B2 respectively. SLMs showed an average of 66.67 – 83.3% oedema inhibition, while the reference had 50%, and ulcer inhibition of 75% for batch D1. Conclusion: Due to the good properties exhibited by the aspirin-loaded SLMS, they could be used for the treatment of inflammation.
VL  - 7
IS  - 4
ER  -

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Author Information

Chekwube Andrew Ezegbe

Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria
Salome Amarachi Chime

Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria
Lydia Onyinyechi Ugorji

Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria
Calister Elochukwu Ugwu

Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria
Amarachi Kalu Agu

Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria
Oluebube Chisom Onyia

Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria
Godswill Onunkwo

Department of Pharmaceutical Technology and Industrial Pharmacy, Faculty of Pharmaceutical Sciences, University of Nigeria, Nsukka, Nigeria

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APA Style

Chekwube Andrew Ezegbe, Salome Amarachi Chime, Lydia Onyinyechi Ugorji, Calister Elochukwu Ugwu, Amarachi Kalu Agu, et al. (2021). Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids. American Journal of Biological and Environmental Statistics, 7(4), 94-103. https://doi.org/10.11648/j.ajbes.20210704.14

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ACS Style

Chekwube Andrew Ezegbe; Salome Amarachi Chime; Lydia Onyinyechi Ugorji; Calister Elochukwu Ugwu; Amarachi Kalu Agu, et al. Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids. Am. J. Biol. Environ. Stat. 2021, 7(4), 94-103. doi: 10.11648/j.ajbes.20210704.14

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AMA Style

Chekwube Andrew Ezegbe, Salome Amarachi Chime, Lydia Onyinyechi Ugorji, Calister Elochukwu Ugwu, Amarachi Kalu Agu, et al. Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids. Am J Biol Environ Stat. 2021;7(4):94-103. doi: 10.11648/j.ajbes.20210704.14

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@article{10.11648/j.ajbes.20210704.14,
  author = {Chekwube Andrew Ezegbe and Salome Amarachi Chime and Lydia Onyinyechi Ugorji and Calister Elochukwu Ugwu and Amarachi Kalu Agu and Oluebube Chisom Onyia and Godswill Onunkwo},
  title = {Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids},
  journal = {American Journal of Biological and Environmental Statistics},
  volume = {7},
  number = {4},
  pages = {94-103},
  doi = {10.11648/j.ajbes.20210704.14},
  url = {https://doi.org/10.11648/j.ajbes.20210704.14},
  eprint = {https://article.sciencepublishinggroup.com/pdf/10.11648.j.ajbes.20210704.14},
  abstract = {Background: PEGylation is a strategy that on therapeutic molecules such as drugs, proteins and macromolecules, in order to improve their delivery. It has this unique property of increasing the size and molecular weight of biomolecules that are conjugated in nature in order to improve water solubility, reduction in renal clearance and protects the drug from enzymatic degradation. Objectives: The objectives of this work was to formulate sustained release aspirin-loaded solid lipid microparticles based on PEGylated lipid matrix, to evaluate the in-vitro properties of the SLM and to study the anti-inflammatory and ulcerogenic properties of the SLM. Methods: Aspirin-loaded solid lipid microparticles (SLMs) were formulated by cold homogenization method. Furthermore, they were analyzed for the encapsulation efficiency, in-vitro release, particle size, anti-inflammatory and ulcer inhibition properties. Results: Particle size ranged from 9.36±2.63 to 16.77±5.80 µm for batches B1 to D1 SLMs loaded with 10% LM, 5% PEG 4000 and 0.25-1% aspirin respectively, while batches B2 to D2 formulated with 10% LM, 10% PEG and 0.25 -1% aspirin had particle size range of 9.09±4.03 to 15.71±10.09 µm. Batches D1 containing 1% of aspirin had the highest encapsulation efficiency of 58%. Maximum in-vitro release of 29.20% and 15.85% were obtained at 6 h for batches D1 and B2 respectively. SLMs showed an average of 66.67 – 83.3% oedema inhibition, while the reference had 50%, and ulcer inhibition of 75% for batch D1. Conclusion: Due to the good properties exhibited by the aspirin-loaded SLMS, they could be used for the treatment of inflammation.},
 year = {2021}
}

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TY  - JOUR
T1  - Formulation Design and in vitro-in vivo Evaluation of Sustained Release Aspirin Microparticles Based on PEGylated Lipids
AU  - Chekwube Andrew Ezegbe
AU  - Salome Amarachi Chime
AU  - Lydia Onyinyechi Ugorji
AU  - Calister Elochukwu Ugwu
AU  - Amarachi Kalu Agu
AU  - Oluebube Chisom Onyia
AU  - Godswill Onunkwo
Y1  - 2021/12/02
PY  - 2021
N1  - https://doi.org/10.11648/j.ajbes.20210704.14
DO  - 10.11648/j.ajbes.20210704.14
T2  - American Journal of Biological and Environmental Statistics
JF  - American Journal of Biological and Environmental Statistics
JO  - American Journal of Biological and Environmental Statistics
SP  - 94
EP  - 103
PB  - Science Publishing Group
SN  - 2471-979X
UR  - https://doi.org/10.11648/j.ajbes.20210704.14
AB  - Background: PEGylation is a strategy that on therapeutic molecules such as drugs, proteins and macromolecules, in order to improve their delivery. It has this unique property of increasing the size and molecular weight of biomolecules that are conjugated in nature in order to improve water solubility, reduction in renal clearance and protects the drug from enzymatic degradation. Objectives: The objectives of this work was to formulate sustained release aspirin-loaded solid lipid microparticles based on PEGylated lipid matrix, to evaluate the in-vitro properties of the SLM and to study the anti-inflammatory and ulcerogenic properties of the SLM. Methods: Aspirin-loaded solid lipid microparticles (SLMs) were formulated by cold homogenization method. Furthermore, they were analyzed for the encapsulation efficiency, in-vitro release, particle size, anti-inflammatory and ulcer inhibition properties. Results: Particle size ranged from 9.36±2.63 to 16.77±5.80 µm for batches B1 to D1 SLMs loaded with 10% LM, 5% PEG 4000 and 0.25-1% aspirin respectively, while batches B2 to D2 formulated with 10% LM, 10% PEG and 0.25 -1% aspirin had particle size range of 9.09±4.03 to 15.71±10.09 µm. Batches D1 containing 1% of aspirin had the highest encapsulation efficiency of 58%. Maximum in-vitro release of 29.20% and 15.85% were obtained at 6 h for batches D1 and B2 respectively. SLMs showed an average of 66.67 – 83.3% oedema inhibition, while the reference had 50%, and ulcer inhibition of 75% for batch D1. Conclusion: Due to the good properties exhibited by the aspirin-loaded SLMS, they could be used for the treatment of inflammation.
VL  - 7
IS  - 4
ER  -

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