Lipid Nanoparticles Improve the Uptake of α-Asarone Into the Brain Parenchyma: Formulation, Characterization, In Vivo Pharmacokinetics, and Brain Delivery
Abstract Treatment of brain-related diseases is one of the most strenuous challenges in drug delivery research due to numerous hurdles, including poor blood-brain barrier penetration, lack of specificity, and severe systemic toxicities. Our research primarily focuses on the delivery of natural therapeutic compound, α-asarone, for the treatment of brain-related diseases. However, α-asarone has poor aqueous solubility, bioavailability, and stability, all of which are critical issues that need to be addressed. This study aims at formulating a lipid nanoparticulate system of α-asarone (A-LNPs) that could be used as a brain drug delivery system. The physicochemical, solid-state properties, stability, and in vitro and in vivo studies of the A-LNPs were characterized. The release of α-asarone from the A-LNPs was prolonged and sustained. After intravenous administration of A-LNPs or free α-asarone, significantly higher levels of α-asarone from the A-LNPs were detected in murine plasma and brain parenchyma fractions, confirming the ability of A-LNPs to not only maintain a therapeutic concentration of α-asarone in the plasma, but also transport α-asarone across the blood-brain barrier. These findings confirm that lipid nanoparticulate systems enable penetration of natural therapeutic compound α-asarone through the blood-brain barrier and may be a candidate for the treatment of brain-related diseases..
Medienart: |
E-Artikel |
---|
Erscheinungsjahr: |
2020 |
---|---|
Erschienen: |
2020 |
Enthalten in: |
Zur Gesamtaufnahme - volume:21 |
---|---|
Enthalten in: |
AAPS PharmSciTech - 21(2020), 8 vom: 02. Nov. |
Sprache: |
Englisch |
---|
Beteiligte Personen: |
Ramalingam, Prakash [VerfasserIn] |
---|
Links: |
Volltext [lizenzpflichtig] |
---|
BKL: |
---|
doi: |
10.1208/s12249-020-01832-8 |
---|
funding: |
|
---|---|
Förderinstitution / Projekttitel: |
|
PPN (Katalog-ID): |
SPR041761588 |
---|
LEADER | 01000caa a22002652 4500 | ||
---|---|---|---|
001 | SPR041761588 | ||
003 | DE-627 | ||
005 | 20230519140207.0 | ||
007 | cr uuu---uuuuu | ||
008 | 201103s2020 xx |||||o 00| ||eng c | ||
024 | 7 | |a 10.1208/s12249-020-01832-8 |2 doi | |
035 | |a (DE-627)SPR041761588 | ||
035 | |a (SPR)s12249-020-01832-8-e | ||
040 | |a DE-627 |b ger |c DE-627 |e rakwb | ||
041 | |a eng | ||
082 | 0 | 4 | |a 610 |q ASE |
084 | |a 44.40 |2 bkl | ||
100 | 1 | |a Ramalingam, Prakash |e verfasserin |4 aut | |
245 | 1 | 0 | |a Lipid Nanoparticles Improve the Uptake of α-Asarone Into the Brain Parenchyma: Formulation, Characterization, In Vivo Pharmacokinetics, and Brain Delivery |
264 | 1 | |c 2020 | |
336 | |a Text |b txt |2 rdacontent | ||
337 | |a Computermedien |b c |2 rdamedia | ||
338 | |a Online-Ressource |b cr |2 rdacarrier | ||
520 | |a Abstract Treatment of brain-related diseases is one of the most strenuous challenges in drug delivery research due to numerous hurdles, including poor blood-brain barrier penetration, lack of specificity, and severe systemic toxicities. Our research primarily focuses on the delivery of natural therapeutic compound, α-asarone, for the treatment of brain-related diseases. However, α-asarone has poor aqueous solubility, bioavailability, and stability, all of which are critical issues that need to be addressed. This study aims at formulating a lipid nanoparticulate system of α-asarone (A-LNPs) that could be used as a brain drug delivery system. The physicochemical, solid-state properties, stability, and in vitro and in vivo studies of the A-LNPs were characterized. The release of α-asarone from the A-LNPs was prolonged and sustained. After intravenous administration of A-LNPs or free α-asarone, significantly higher levels of α-asarone from the A-LNPs were detected in murine plasma and brain parenchyma fractions, confirming the ability of A-LNPs to not only maintain a therapeutic concentration of α-asarone in the plasma, but also transport α-asarone across the blood-brain barrier. These findings confirm that lipid nanoparticulate systems enable penetration of natural therapeutic compound α-asarone through the blood-brain barrier and may be a candidate for the treatment of brain-related diseases. | ||
700 | 1 | |a Ganesan, Palanivel |e verfasserin |4 aut | |
700 | 1 | |a Prabakaran, D. S. |e verfasserin |4 aut | |
700 | 1 | |a Gupta, Pardeep K. |e verfasserin |4 aut | |
700 | 1 | |a Jonnalagadda, Sriramakamal |e verfasserin |4 aut | |
700 | 1 | |a Govindarajan, Karthivashan |e verfasserin |4 aut | |
700 | 1 | |a Vishnu, Revuri |e verfasserin |4 aut | |
700 | 1 | |a Sivalingam, Kalaiselvi |e verfasserin |4 aut | |
700 | 1 | |a Sodha, Srushti |e verfasserin |4 aut | |
700 | 1 | |a Choi, Dong-Kug |e verfasserin |4 aut | |
700 | 1 | |a Ko, Young Tag |e verfasserin |4 aut | |
773 | 0 | 8 | |i Enthalten in |t AAPS PharmSciTech |d New York, NY : Springer, 2000 |g 21(2020), 8 vom: 02. Nov. |w (DE-627)SPR02478785X |w (DE-600)2052070-0 |x 1530-9932 |7 nnns |
773 | 1 | 8 | |g volume:21 |g year:2020 |g number:8 |g day:02 |g month:11 |
856 | 4 | 0 | |u https://dx.doi.org/10.1208/s12249-020-01832-8 |z lizenzpflichtig |3 Volltext |
912 | |a GBV_USEFLAG_A | ||
912 | |a GBV_SPRINGER | ||
912 | |a SSG-OLC-PHA | ||
912 | |a SSG-OPC-PHA | ||
912 | |a SSG-OPC-ASE | ||
936 | b | k | |a 44.40 |q ASE |
951 | |a AR | ||
952 | |d 21 |j 2020 |e 8 |b 02 |c 11 |