Enhanced permeability of blood–brain barrier and targeting function of brain via borneol-modified chemically solid lipid nanoparticle

Abstract

IntroductionThe incidence of central nervous system disease has increased in recent years. However, the transportation of drug is restricted by the blood–brain barrier, contributing to the poor therapeutic effect in the brain. Therefore, the development of a new brain-targeting drug delivery system has become the hotspot of pharmacy.Materials and methodsBorneol, a simple bicyclic monoterpene extracted from Dryobalanops aromatica, can direct drugs to the upper body parts according to the theory of traditional Chinese medicine. Dioleoyl phosphoethanolamine (DOPE) was chemically modified by borneol as one of the lipid materials of solid lipid nanoparticle (SLN) in the present study.ResultsThe borneol-modified chemically solid lipid nanoparticle (BO-SLN/CM), borneol-modified physically solid lipid nanoparticle (BO-SLN/PM), and SLN have similar diameter (of about 87 nm) and morphological characteristics. However, BO-SLN/CM has a lower cytotoxicity, higher cell uptake, and better blood–brain barrier permeability compared with BO-SLN/PM and SLN. BO-SLN/CM has a remarkable targeting function to the brain, while BO-SLN/ PM and SLNs are concentrated at the lung.ConclusionThe present study provides an excellent drug delivery carrier, BO-SLN/CM, having the application potential of targeting to the brain and permeating to the blood–brain barrier.

Pep-1&Borneol-Bifunctionalized Carmustin-Loaded Micelles Enhance Anti-Glioma Efficacy through Tumor Targeting and BBB Penetrating

“…As shown in Figure 3B, Bor/C6-M and Pep-1/Bor/C6-M showed significantly higher endocytosis by HBMEC cells than the C6-M group, suggesting that borneol modification was of great importance to improve cellular uptake [24]. However, (about 7.8 × 10 7 cm/s), which was significantly higher than that of CMS-M, suggesting that borneol modification is more effective for BBB penetration [14]. As expected, no significant difference was observed between Bor/C6-M and Pep-1/Bor/C6-M, suggesting that the main contribution of Pep-1 is to recognize tumor cells and enhance internalization, and that of borneol is to enhance the ability to penetrate the BBB and to enhance the uptake by tumor cells to some extent.…”

“…As reported previously [14], 1×10 5 was calculated as follows, Papp = dQ/dt/SC, where dQ/dt represents the transport ratio, S represents the area of membrane, and C represents the initial concentration of CMS.…”

“…Huang et al tested the distribution of borneol after a single injection and confirmed that its localization in the brain tissue was much higher than in other tissues [13]. Zheng et al modified borneol with nano-structured lipid carriers, significantly improving the delivery efficiency of drugs in the brain [14]. These reports suggest that using borneol as a BBB permeation-promoting functional group effectively improves the intracerebral delivery of nanodrugs.…”

Malay Camphor In Arabic Text And Its Latest Trend Of Research

“…And the third is from Japan which considers the particular camphor as among medicinal herbs in Japanese tradition (Ito et al, 2016). However, it is learnt that the one extracted from Dryobalanops aromatica can direct drugs to the upper body parts according to TCM's theory (Chen et al, 2016;Song et al, 2018;Zou et al, 2017). Moreover, it has been acknowledged to attenuate Alzheimer's disease, stroke, cerebral ischemia, cerebritis, and cerebral edema (Yu et al, 2017).…”

<p>Recent expansions of novel strategies towards the drug targeting into the brain</p>

“…Such as, polysorbate coated nanoparticle enters into the brain via the capillary wall through the low-density lipoprotein (LDL) receptor. 67 Owing to the smaller size, it can easily penetrate the cellular layers and target the drug to the specific site. 68,69 The PLA coated nanoparticle shows enhanced drug transport to the brain via the intranasal route.…”