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Repurposing ibuprofen-loaded microemulsion for the management of Alzheimer's disease: evidence of potential intranasal brain targeting.
Drug Deliv. 2021 Dec; 28(1):1188-1203.DD

Abstract

Studies have shown the use of non-steroidal anti-inflammatory drugs, such as ibuprofen could reduce the risk of Alzheimer's disease. The drug-repurposing strategy offers a bright opportunity for these patients. Intranasal administration through the olfactory pathway provides noninvasive and direct drug delivery to the target brain. A novel ibuprofen microemulsion was prepared, characterized and assessed the brain uptake in rats. The solubility of ibuprofen in various oils, surfactants, co-surfactants, and different ratios of surfactant/co-surfactant mixtures was screened and the phase diagrams were constructed. The colloidal particle size was 166.3 ± 2.55 nm and the zeta potential was -22.7 mV. Conductivity and dilution test identified an O/W type microemulsion with pH 4.09 ± 0.08. The rheological study showed a Newtonian flow behavior with cP 10.633 ± 0.603 (mPa⋅s). A steady drug release and linear permeation profiles were observed and showed a 90% permeation rate from the released drug. Ibuprofen microemulsion showed excellent stability in 3-months accelerated storage conditions, heating-cooling and freeze-thaw cycles, accelerated centrifugation, and 6- and 12-months long-term storage conditions. In vivo studies in rats further demonstrated a 4-fold higher brain uptake of ibuprofen from the microemulsion compared to the reference solution and nearly 4-fold and 10-fold higher compared to the intravenous and oral administrations. This study provides an exciting repurposing strategy and new administration route for the treatment of Alzheimer's disease.

Authors+Show Affiliations

Department of Pharmaceutics & Pharmaceutical Technology, Pharos University in Alexandria, Alexandria, Egypt.Department of Pharmaceutics & Pharmaceutical Technology, Pharos University in Alexandria, Alexandria, Egypt.Department of Pharmaceutics, Alexandria University, Alexandria, Egypt.Department of Pharmaceutics, Alexandria University, Alexandria, Egypt.

Pub Type(s)

Journal Article

Language

eng

PubMed ID

34121565

Citation

Wen, Ming Ming, et al. "Repurposing Ibuprofen-loaded Microemulsion for the Management of Alzheimer's Disease: Evidence of Potential Intranasal Brain Targeting." Drug Delivery, vol. 28, no. 1, 2021, pp. 1188-1203.
Wen MM, Ismail NIK, Nasra MMA, et al. Repurposing ibuprofen-loaded microemulsion for the management of Alzheimer's disease: evidence of potential intranasal brain targeting. Drug Deliv. 2021;28(1):1188-1203.
Wen, M. M., Ismail, N. I. K., Nasra, M. M. A., & El-Kamel, A. H. (2021). Repurposing ibuprofen-loaded microemulsion for the management of Alzheimer's disease: evidence of potential intranasal brain targeting. Drug Delivery, 28(1), 1188-1203. https://doi.org/10.1080/10717544.2021.1937383
Wen MM, et al. Repurposing Ibuprofen-loaded Microemulsion for the Management of Alzheimer's Disease: Evidence of Potential Intranasal Brain Targeting. Drug Deliv. 2021;28(1):1188-1203. PubMed PMID: 34121565.
* Article titles in AMA citation format should be in sentence-case
TY - JOUR T1 - Repurposing ibuprofen-loaded microemulsion for the management of Alzheimer's disease: evidence of potential intranasal brain targeting. AU - Wen,Ming Ming, AU - Ismail,Noha Ismail Khamis, AU - Nasra,Maha M A, AU - El-Kamel,Amal Hassan, PY - 2021/6/14/entrez PY - 2021/6/15/pubmed PY - 2021/11/18/medline KW - Alzheimer’s disease KW - Repurposing KW - brain targeting KW - ibuprofen KW - intranasal delivery KW - microemulsion SP - 1188 EP - 1203 JF - Drug delivery JO - Drug Deliv VL - 28 IS - 1 N2 - Studies have shown the use of non-steroidal anti-inflammatory drugs, such as ibuprofen could reduce the risk of Alzheimer's disease. The drug-repurposing strategy offers a bright opportunity for these patients. Intranasal administration through the olfactory pathway provides noninvasive and direct drug delivery to the target brain. A novel ibuprofen microemulsion was prepared, characterized and assessed the brain uptake in rats. The solubility of ibuprofen in various oils, surfactants, co-surfactants, and different ratios of surfactant/co-surfactant mixtures was screened and the phase diagrams were constructed. The colloidal particle size was 166.3 ± 2.55 nm and the zeta potential was -22.7 mV. Conductivity and dilution test identified an O/W type microemulsion with pH 4.09 ± 0.08. The rheological study showed a Newtonian flow behavior with cP 10.633 ± 0.603 (mPa⋅s). A steady drug release and linear permeation profiles were observed and showed a 90% permeation rate from the released drug. Ibuprofen microemulsion showed excellent stability in 3-months accelerated storage conditions, heating-cooling and freeze-thaw cycles, accelerated centrifugation, and 6- and 12-months long-term storage conditions. In vivo studies in rats further demonstrated a 4-fold higher brain uptake of ibuprofen from the microemulsion compared to the reference solution and nearly 4-fold and 10-fold higher compared to the intravenous and oral administrations. This study provides an exciting repurposing strategy and new administration route for the treatment of Alzheimer's disease. SN - 1521-0464 UR - https://www.unboundmedicine.com/medline/citation/34121565/Repurposing_ibuprofen_loaded_microemulsion_for_the_management_of_Alzheimer's_disease:_evidence_of_potential_intranasal_brain_targeting_ L2 - https://www.tandfonline.com/doi/full/10.1080/10717544.2021.1937383 DB - PRIME DP - Unbound Medicine ER -