With all this earlier research on rapamycin for stroke I bet our incompetent stroke medical 'professionals' have done ABSOLUTELY NOTHING! Aren't you glad they are so fucking incompetent that your children and grandchildren won't recover from a stroke? It took me all of two minutes to Google Scholar for 'rapamycin for stroke' and find all this; and I'm obviously stroke-addled and know nothing!
Transferrin and Borneol-Enhanced Liposomes for Targeted Rapamycin Delivery in TBI
Authors Cai S, Yuan Z, Chen Y, Gong M, Lai J, Yan P, Mei Z
Received 29 July 2024
Accepted for publication 28 February 2025
Published 11 April 2025 Volume 2025:20 Pages 4503—4518
DOI https://doi.org/10.2147/IJN.S489165
Checked for plagiarism Yes
Review by Single anonymous peer review
Peer reviewer comments 2
Editor who approved publication: Dr Kamakhya Misra
Shihong Cai,1,2,* Zhongwen Yuan,1,* Yanfang Chen,3 Mingjie Gong,1 Jianqi Lai,1 Pengke Yan,1 Zhengrong Mei1
1Department
of Pharmacy, Guangdong Provincial Key Laboratory of Major Obstetric
Diseases, Guangdong Provincial Clinical Research Center for Obstetrics
and Gynecology, The Third Affiliated Hospital, Guangzhou Medical
University, Guangzhou, People’s Republic of China; 2Zhanjiang Healthcare Security Service Management Center, Zhanjiang, People’s Republic of China; 3Department of Pharmacy, Guangzhou Eighth People’s Hospital, Guangzhou Medical University, Guangzhou, People’s Republic of China
*These authors contributed equally to this work
Correspondence: Pengke Yan, Email gysyypk@126.com Zhengrong Mei, Email meizhengrong@126.com
Background:
The therapeutic potential of rapamycin (RAPA) for traumatic brain
injury (TBI) is limited by its low bioavailability and poor penetration
across the blood-brain barrier (BBB). We developed transferrin-modified
rapamycin and borneol co-delivery liposomes (TF-RAPA/BO-LIP) to overcome
these barriers, aiming to enhance both drug delivery to the brain and
the treatment efficacy.
Methods: We employed the
emulsion-solvent evaporation method to prepare TF-RAPA/BO-LIP and
characterized their particle size, zeta potential, morphology,
stability, and encapsulation efficiency. Pharmacokinetic studies were
conducted in SD rats, and drug concentration was analyzed using
LC-MS/MS. The brain-targeting capability and therapeutic efficacy were
evaluated through in vitro cellular uptake studies, and in vivo in a TBI
mouse model using both neurological and cognitive assessments.
Results:
TF-RAPA/BO-LIP displayed optimal characteristics (95 nm particle size,
> 90% encapsulation efficiency) and demonstrated enhanced stability.
Pharmacokinetic analyses revealed reduced drug clearance and increased
drug concentration-time curve area, indicating improved systemic and
brain-specific drug bioavailability. Notably, TF-RAPA/BO-LIP achieved
significantly higher RAPA accumulation in the brain tissue. Importantly,
treatment with TF-RAPA/BO-LIP significantly ameliorated neurological
deficits and improved spatial memory in TBI mice, as evidenced by
behavioral tests.
Conclusion: Our study highlights
TF-RAPA/BO-LIP as a promising strategy for delivering RAPA across the
BBB, substantially enhancing its therapeutic efficacy for TBI. This
novel liposomal system not only improves RAPA bioavailability but also
offers significant neuroprotection, potentially transforming the
clinical management of TBI.
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