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Temporally increasing blood-brain barrier permeability?

bbb gintonin tcm bornrol

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#1 Metagene

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Posted 20 July 2014 - 12:55 AM


I causally looked into different ways of accomplishing this for the heck of it. LPA and E-Cadherin peptide might be a viable
solutions but I want to know if comparable results can be obtain preferably thru oral administration.

Rapid and reversible enhancement of blood-brain barrier permeability using lysophosphatidic acid.

AuthorsOn NH, et al. Show allJournal
J Cereb Blood Flow Metab. 2013 Dec;33(12):1944-54. doi: 10.1038/jcbfm.2013.154. Epub 2013 Sep 18.
Affiliation
Abstract
The present study characterizes the effects of lysophosphatidic acid (LPA) on blood-brain barrier (BBB) permeability focusing specifically on the time of onset, duration, and magnitude of LPA-induced changes in cerebrovascular permeability in the mouse using both magnetic resonance imaging (MRI) and near infrared fluorescence imaging (NIFR). Furthermore, potential application of LPA for enhanced drug delivery to the brain was also examined by measuring the brain accumulation of radiolabeled methotrexate. Exposure of primary cultured brain microvessel endothelial cells (BMECs) to LPA produced concentration-dependent increases in permeability that were completely abolished by clostridium toxin B. Administration of LPA disrupted BBB integrity and enhanced the permeability of small molecular weight marker gadolinium diethylenetriaminepentaacetate (Gd-DTPA) contrast agent, the large molecular weight permeability marker, IRdye800cwPEG, and the P-glycoprotein efflux transporter probe, Rhodamine 800 (R800). The increase in BBB permeability occurred within 3 minutes after LPA injection and barrier integrity was restored within 20 minutes. A decreased response to LPA on large macromolecule BBB permeability was observed after repeated administration. The administration of LPA also resulted in 20-fold enhancement of radiolabeled methotrexate in the brain. These studies indicate that administration of LPA in combination with therapeutic agents may increase drug delivery to the brain.

Modulation of Blood-Brain Barrier Permeability in Mice Using Synthetic E-Cadherin Peptide.

http://www.ncbi.nlm....4045401/related


It's should be noted Gintonin also functions as a selective LPA receptor agonist.

Gintonin: a novel ginseng-derived ligand that targets G protein- coupled lysophosphatidic acid receptors.

Authors
Nah SY.
Journal
Curr Drug Targets. 2012 Dec;13(13):1659-64.

Affiliation
Abstract
Ginseng, the root of Panax ginseng C.A. Meyer, is one of the oldest herbal medicines and induces a variety of physiological and pharmacological effects. Ginseng contains saponins called ginsenosides, which are considered as the biologically active ingredients in ginseng. Increasing evidences indicate that ginsenosides are non-selective in their actions and high concentrations are required for cellular effects. Crude ginseng total saponin (cGTS) fraction is about 50% ginsenoside in composition, but the remainder is not defined clearly. Biochemically, cGTS fraction triggers differing patterns of ginsenoside activity; for example, the cGTS fraction itself functions as an agent that activates a G protein-coupled receptor because it induces endogenous calcium (Ca2+)-activating chloride (Cl-) channel activations in Xenopus oocytes via the same signaling pathways used by Gαq/11 protein-coupled receptors. Recent reports have revealed that the cGTS fraction contains novel glycolipoproteins, designated the gintonin. It was discovered that gintonin, but not ginsenosides, interacts with unidentified membrane proteins to generate [Ca2+]i transient in mammalian cells and to activate endogenous Ca2+-activating Cl- channels in Xenopus oocytes. Further studies have shown that gintonin is a novel lysophosphatidic acids (LPAs)-ginseng protein complex and can selectively activate LPA receptors with an affinity greater than that of LPA. This review aims to characterize gintonin as an LPA receptor ligand, explain the reasons why gintonin remained unidentified for a long time, list the advantages of LPA-ginseng protein complexes over free LPAs, compare the activities of gintonin and ginsenoside, and describe the pharmacological applications of gintonin as a drug that targets LPA receptors.

http://www.ncbi.nlm....3161173/related

Worth reading

Gintonin, newly identified compounds from ginseng, is novel lysophosphatidic acids-protein complexes and activates G protein-coupled lysophosphatidic acid receptors with high affinity.

http://www.ncbi.nlm....3717094/related

Gintonin, a ginseng-derived novel ingredient, evokes long-term potentiation through N-methyl-D-aspartic acid receptor activation: involvement of LPA receptors.

http://www.ncbi.nlm....2286231/related

Edited by Metagene, 20 July 2014 - 01:49 AM.


#2 Metagene

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Posted 20 July 2014 - 03:07 AM

Okay this is a better starting point. Neuroprotective while simultaneously enhancing blood-brain barrier permeability? Enter Borneol.

Research of bornrol promote drugs through blood-brain barrier].

AuthorsLv X, et al. Show allJournal
Zhongguo Zhong Yao Za Zhi. 2012 Apr;37(7):878-81. Article in Chinese.
Affiliation
Abstract
Malignant tumor, epilepsy, dementia, cerebral ischemia and other brain diseases have very high rates of disability and mortality. Currently, many drugs are developed to treat such diseases and the effect is obviously. But they can not achieve the purpose to control these diseases because many of the drugs can not pass through the blood-brain barrier (BBB). Therefore, the treatment is not good. Borneol as the represent of the aromatic resuscitation medicine, it has strong fat-soluble active ingredients, small molecular weight, volatile and through the BBB quickly. It can also promote other therapeutic drugs through the BBB. It has two-ways regulations on BBB permeability and the damage of brain tissue is small, this have important theoretical significances and application values.

http://www.ncbi.nlm....=6&from=borneol


The mechanism of the opening of the blood-brain barrier by borneol: A pharmacodynamics and pharmacokinetics combination study.

AuthorsYu B, et al. Show allJournal
J Ethnopharmacol. 2013 Oct 25. pii: S0378-8741(13)00735-6. doi: 10.1016/j.jep.2013.10.028. [Epub ahead of print]

Affiliation
Abstract
ETHNOPHARMACOLOGICAL RELEVANCE: Borneol is widely used in traditional Chinese medicine to facilitate the distribution of central nervous system (CNS) drugs in brain due to its ability to open blood-brain barrier (BBB), however, the underlying mechanism is still unclear. In this study, the effect of borneol on different brain regions were investigated to explore the mechanism.

MATERIALS AND METHODS: After oral administration of borneol (0.1, 0.2g/kg) for seven consecutive days, SD rats were injected with Rh123 (1.0mg/kg). The concentrations of Rh123 were detected in four brain regions of cortex, hippocampus, hypothalamus and striatum by a small animal vivo imaging system and a fluorescence microplate reader respectively. The ultrastructures of BBB were examined. Moreover, the expressions of the four transporters of ATP-binding cassette (ABC) family, multidrug resistance 1a (Mdr1a), multidrug resistance 1b (Mdr1b), multidrug resistance protein 1 (Mrp1), Mrp4, Mrp5 and breast cancer resistance protein (Bcrp) in the four brain regions were analyzed. Finally, the deliveries of borneol in the plasma and the four brain regions were examined by a pharmacokinetics study.

RESULTS: Administration of 0.2g/kg borneol produced loose structure in the tight junction and void structure between the endothelial cell and mesangial cell. Borneol at 0.1g/kg and 0.2g/kg increased the delivery of Rh123 in hippocampus and hypothalamus obviously. Permeability index followed a similar trend. Protein expression assays showed that borneol decreased the expression of Mdr1 and Mrp1 in hippocampus and hypothalamus. Further RT-PCR study showed that borneol decreased the expressions of both Mdr1a and Mdr1b in hippocampus and hypothalamus. The pharmacokinetics study demonstrated that the delivery of borneol in cortex was the most and that in striatum the least, with the deliveries of borneol in hippocampus and hypothalamus in between.

CONCLUSIONS: Borneol showed tissue specific BBB-opening effect, which was associated with its regulation of the ultrastructure of brain tissues and the expressions of Mdr1a, Mdr1b and Mrp1. The present study indicated that borneol should be used in concert with drugs targeting hippocampus or hypothalamus to exert its synergistic effect to the maximum.

http://www.ncbi.nlm....31&from=borneol

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#3 Metagene

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Posted 21 July 2014 - 05:13 PM

Nice, here is a study that demonstrates Borneol's BBB permability enhancing properties using Levodopa.

Borneol Enhanced Permeability of L-DOPA across Blood-brain Barrier - Potential to Lower Dosage of L-DOPA to Treat Parkinson's Disease

Background and aims: Parkinson´s disease (PD) is chronic degenerative diseases of central nervous system that suffered by the elderly. Levodopa (L-DOPA) is one of the commonly prescribed drugs to treat PD. However, less than 1% dosage of L-DOPA passes through the blood-brain barrier (BBB) into brain. Excessive intake of L-DOPA in blood results in various side effects such as end of dose deterioration, peak-dose dyskinesia.
Borneol was found to increase the permeability of BBB. The aim of study is to study the enhancing effect borneol on permeability of L-DOPA through BBB.
Methods: After clinical equivalent dose of L-DOPA (416mg·kg-1) is administered orally by SD rats, oral gavage of serial concentration of borneol is given. Cerebrospinal fluid (CSF) was collected through the foramen magnum using HPLC to determine concentration of L-DOPA. For pharmacokinetic study, CSF was collected at different time points after oral administration of L-DOPA or/and borneol. Various pharmacokinetic parameters of L-DOPA and borneol are assessed.
Result and conclusions: Borneol with 300mg·kg-1 was found maximal concentration of L-DOPA which is 4.5-fold of control in rats CSF (p< 0.01). Borneol enhanced the permeability of L-DOPA across BBB. In pharmacokinetic study, the parameter T1/2, AUC and Cmax increased by 145.0%, 105.8% and 83.1% respectively. It implied that borneol slowed down the metabolism and prolonged the maintenance of effective concentration of L-DOPA in brain. Thus borneol enhanced permeability of L-DOPA across blood-brain-barrier. It is suggested that concurrent in-take of borneol and low dose L-DOPA can be explored to treat Parkinson's disease.

http://adpd.ekonnect...29/program.aspx

Does anyone think borneol could enhance absorption of say Hederagenin!? http://www.longecity...on-hederagenin/

Enhancement of intestinal absorption of akebia saponin D by borneol and probenecid in situ and in vitro.

AuthorsZhou Y, et al. Show allJournal
Environ Toxicol Pharmacol. 2010 May;29(3):229-34. doi: 10.1016/j.etap.2010.01.004. Epub 2010 Jan 29.
Affiliation
Abstract
Akebia saponin D is a typical bioactive triterpenoid saponin isolated the rhizome of Dipsacus asper Wall. Our previous studies demonstrated that the oral bioavailability of akebia saponin D was very low, but the underlying mechanisms remained unknown. The present study aims to investigate the intestinal absorptive characteristics of akebia saponin D as well as the absorptive transport behavior influenced by co-administration of three absorption-enhancing agents and three efflux protein inhibitors using an in vitro everted gut sac method and an in situ intestinal perfusion model. The results showed that akebia saponin D had a quite limited intestinal permeability, and there was a non-linear increase in transepithelial transportation with increasing concentrations of akebia saponin D. The absorption of akebia saponin D was intestinal segment selective and the small intestine was the best absorptive site. Among three absorption promoters, borneol could significantly improve the permeability of akebia saponin D across ileum, while Tween-80 and DMSO had almost no absorption-enhancing effect. In addition, verapamil, probenecid and pantoprazole in the perfusates were used in this study as modulators of transporters such as P-glycoprotein, MRPs and BCRP in the intestinal mucosa, respectively. The results exhibited that the ileal permeability of akebia saponin D was markedly elevated by the co-administration of probenecid, indicating that akebia saponin D may be likely a substrate of MRPs. The above-mentioned results suggest that akebia saponin D has a poor intestinal absorption not only due to its poor transepithelial permeability but also owing to the contribution of efflux transporters such as MRPs in the intestine.

http://www.ncbi.nlm....ubmed/21787607/

Effects of borneol on the intestinal transport and absorption of two P-glycoprotein substrates in rats.

AuthorsHe H, et al. Show allJournal
Arch Pharm Res. 2011 Jul;34(7):1161-70. doi: 10.1007/s12272-011-0714-y. Epub 2011 Aug 3.
Affiliation
Abstract
As the most prevalent route of delivery, oral administration has the challenge of potentially low bioavailability in part because P-glycoprotein (P-gp) in the intestinal tract affects absorption. Therefore, absorption enhancers or P-gp inhibitors are strategies to solve this problem. The aim of the present study was to investigate the effects of borneol on transportation of colchicine and rhodamine123, two P-gp substrates, in rats. In vitro transportation was assessed with a diffusion chamber system with isolated rat intestines. Different concentrations of borneol (10, 40 and 80 μg/mL) were prepared in solutions with two P-gp substrates compared with blank solutions. The in vivo effects on colchicine were assessed by a pharmacokinetic study. Borneol enhanced the absorptive transport of two P-gp substrates, which was relevant to the concentration. A pharmacokinetic study showed that in the presence of borneol, a significant increase in C(max) and AUC(0→8) of colchicine occurred when compared to colchicine alone. The study showed that borneol affected two P-gp substrates in the intestine, possibly by inhibiting the effects of P-gp and enhancing intestinal absorption of drugs. Therefore, borneol could be developed as a P-gp inhibitor and absorptive enhancer.

http://www.ncbi.nlm....ubmed/21811923/

Edited by Metagene, 21 July 2014 - 05:24 PM.


#4 Flex

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Posted 25 July 2014 - 05:07 PM

Intresting.

Borneol could get the new Piperine, so to say.

 

 



#5 StevesPetRat

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Posted 25 July 2014 - 07:20 PM

Mannitol seems like it would be easiest though the oral bioavailability ain't that great.

#6 MizTen

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Posted 25 July 2014 - 07:38 PM

Interesting stuff. Perhaps a mild state of dehydration would increase BBB permeability...

#7 StevesPetRat

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Posted 25 July 2014 - 07:57 PM

Interesting stuff. Perhaps a mild state of dehydration would increase BBB permeability...


If we're going that route, sleep apnea / hypoxia works too ;)

#8 Metagene

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Posted 26 July 2014 - 12:08 AM

Another compound worthy of potential enhancement: Baicalin 

 

 

 

Baicalin, an emerging multi-therapeutic agent: pharmacodynamics, pharmacokinetics, and considerations from drug development perspectives.
Abstract

Baicalin was extensively researched for utility in a number of therapeutic areas owing to its anti-inflammatory, anti-oxidant, anti-bacterial, and anti-cancer properties. A number of preclinical studies, in vitro work, and mechanistic studies were performed to understand the absorption, distribution, metabolism, and excretion profiles of baicalin. The absorption of baicalin involved several complexities: the restriction to two distant sites; the conversion of baicalin to baicalein; the possible role of transporter(s); and enhanced absorption due to breakdown of conjugates by beta-glucuronidase. Limited distribution data suggest that baicalin reached several sites such as the brain, eye lens, thymus, etc. Hepatobiliary recycling also served as a distribution phase for sustained delivery of baicalin. Metabolism data suggest the rapid conversion of baicalin to baicalein, which was extensively subjected to Phase 2 metabolism, conjugates baicalein glucuronide/sulfate have been identified. Limited excretion data suggest involvement of renal and faecal routes--glucuronide and sulfate conjugates were excreted in urine and faeces (via biliary excretion). The published data on baicalin suggest imminent challenges for developing baicalin and/or during co-administration with other agents. These challenges are absorption related (transporter or changes in the microenvironment), metabolism related (CYP2B6 induction and/or CYP2E1 inhibition), and excretion/efflux related (competitive biliary pathway and/or OATP1B1 transport).

 

 

 

 

 

http://www.ncbi.nlm....pubmed/20230189

 

 

 

Enhancing effects of absorption enhancers on in situ nasal absorption of baicalin
HUANG Hui-feng,ZHANG Miao,TANG Xing(School of pharmacy,Shenyang Pharmaceutical University,Shenyang 110016,China)  
Objective To investigate the nasal absorption of baicalin and the enhancing activities of several absorption enhancers.Methods Nasal circulatory perfusion test in situ was employed to investigate the effects of absorption enhancers for nasal mucosa absorption of baicalin in rats.And the enchancing activities were evaluated by first-order nasal absorption rate constant k.Results Absorption enhancers were necessary to facilitate baicalin absorption by nasal mucosa.Among the absorption enhancers,the order of increasing absorption of baicalin caused by the enhancers was:1% sodium deoxycholate 0.5% chitosan≈0.5% borneol≈5% methyl-β-cyclodextrin5% HP-βCD5% β-CD1% Tween-80≈0.1% EDTA-Na2≈1% lecithin.Conclusions 0.5% chitosan,0.5% borneol,5% methyl-β-cyclodextrin and 5% HP-β-CD are the promising candidates with good enhancing activities for nasal baicalin delivery.

 

http://en.cnki.com.c...YD200805002.htm

 
Anti-bacterial Synergistic Effects of Baicalin and Borneol on Staphylococcus epidermidis
YU Yue1,WANG Ya-jing1,PI Jia-xin1,WANG Dong-heng2,XUAN Xiao-yu1,ZHENG Yin1(1.Tianjin University of Traditional Chinese Medicine,Tianjin State Key Laboratory of Modern Chinese Medicine,Tianjin 300193,China;2.Tianjin Zhongyi Pharmaceutical Co.Ltd.,Tianjin 300193,China)  
Objective: The aim of this paper is to estimate the anti-bacterial effects of baicalin and borneol on Staphylococcus epidermidis.Method: A modified turbidimetry,which referred to the solution absorbance assay at 600 nm,was applied to determine the inhibition ratio of S.epidermidis growth by adding different concentrations of baicalin,borneol and baicalin-borneol mixed solutions.Result: The inhibition ratios of S.epidermidis growth of different baicalin concentration solutions with borneol added showed significant increase compared with blank baicalin solutions.The inhibition ratios were 49.78% with 1 200 mg.L-1 baicalin solution,and 13.41% with 600 mg.L-1borneol solution,separately.The significant inhibition ratio which indicated the synergistic effect was 78.15% under the mixed solution with the baicalin concentration of 1200 mg.L-1 and borneol 600 mg.L-1.Conclusion: The compatibility of a certain amount of baicalin and borneol,which significantly enhanced the anti-bacterial effects of two compounds separately,indicated the outstanding synergistic effect on the inhibition of S.epidermidis growth.

 

 

 

http://en.cnki.com.c...FX201310056.htm

 

Side note: Baicalin when used alone can actually decrease BBB permeability in certain conditions

 

 

 

Baicalin attenuates brain edema in a rat model of intracerebral hemorrhage.
Abstract

Baicalin is a flavonoid compound purified from the roots of Scutellaria baicalensis, which possesses multiple biological activities. Previous studies have shown that baicalin is protective in ischemic cerebral diseases. The aim of the present study was to examine the effects of baicalin on braininjury in a rat model of intracerebral hemorrhage (ICH) and to explore the possible mechanisms. Intracerebral hemorrhage was induced in male Wistar rats by injection of 0.5 U collagenaseVII to the caudate nucleus. Sham operation rats were injected with equal volume of saline. After the induction of ICH, the rats were randomly divided into four groups and administered with different dose of baicalin (0, 25, 50, or 100 mg/kg in saline) through peritoneal injection. The brain tissues around the hemorrhage areas were collected on days 1, 3, and 5 after treatment. Brain edema was analyzed by desiccation method; the metalloproteinase-9 (MMP-9) protein and mRNA expression were determined by western blotting and real time RT-PCR, respectively. Nuclear factor-κB (NF-κB) protein expression was analyzed by western blotting. IL-1β and IL-6 levels were determined by enzyme-linked immunosorbent assay. Blood-brain barrier permeability was determined by Evans blue leakage method. The results showed that baicalin reducedbrain edema following ICH in a dose-dependent manner, with concomitant inhibition of NF-κB activation and suppression of MMP-9 expression. In addition, baicalin also reduced IL-1β and IL-6 production, as well as blood-brain barrier permeability. The above results indicated that baicalin prevents against perihematomal edema development after intracerebral hemorrhage possibly through an anti-inflammatory mechanism.

 

 
Effect of baicalin on matrix metalloproteinase-9 expression and blood-brain barrier permeability following focal cerebral ischemia in rats.
Abstract

Focal cerebral ischemia results in an increased expression of matrix metalloproteinase-9 (MMP-9), which induces vasogenic brain edema via disrupting the blood-brain barrier (BBB) integrity. Recent studies from our laboratory showed that baicalin reduces ischemic brain damage by inhibiting inflammatory reaction and neuronal apoptosis in a rat model of focal cerebral ischemia. In the present study, we first explored the effect ofbaicalin on the neuronal damage, brain edema and BBB permeability, then further investigated its potential mechanisms. Sprague-Dawley rats underwent permanent middle cerebral artery occlusion (MCAO). Baicalin was administrated by intraperitoneally injected twice at 2 and 12 h after the onset of MCAO. Neuronal damage, brain edema and BBB permeability were measured 24 h following MCAO. Expression of MMP-9 protein and mRNA were determined by western blot and RT-PCR, respectively. Expression of tight junction protein (TJP) occludin was detected by western blot. Neuronal damage, brain edema and BBB permeability were significantly reduced by baicalin administration following focal cerebral ischemia. Elevated expression of MMP-9 protein and mRNA were significantly down-regulated by baicalin administration. In addition, MCAO caused the decreased expression of occludin, which was significantly up-regulated by baicalin administration. Our study suggested that baicalin reduces MCAO-induced neuronal damage, brain edema and BBB permeability, which might be associated with the inhibition of MMP-9

 

 

 

 

 

http://www.ncbi.nlm....d brain barrier

 

Percutaneous absorption effects of Chinese herbal medicine
 
Yongzhan Bao1,2, Shaohua Zhang1,2 and Wanyu Shi1,2*
1College of Veterinary Medicine, Agricultural University of Hebei, Baoding 071001, China.
2
Institute of Traditional Chinese Veterinary Medicine, Agricultural University of Hebei, China.
Accepted 12 December, 2011
This study was carried out to evaluate the effects of Chinese herbal transdermal ointment on mastitis in 
the dairy cow and to select the best efficient formula for treating the disorder. With chlorogenic acid as 
a marker, using high performance liquid chromatography (HPLC), the contents of chlorogenic acid in 
permeate liquid were determined. Different skin permeation enhancing effects of Chinese herbal 
medicinal formulations and various herbal transdermal promoters were evaluated in the form of 
ointment. The results indicated that ultrafined powder (UFP) of Chinese herbal medicine (CHM) directly 
adding to medication and 4.5% borneol plus 4.5% Azone as skin permeation enhancers showed the 
best skin-penetrating effect
 
 
 
Ordinarily, combination of two or more transdermal 
promoters works synergistically in promoting drug

penetration through the skin with much better results than 

one promotor alone. Thereby, combined use of 
promoters will reduce the amount used of each promoter 
with lower toxicity. Nitrogen ketones and borneol are the 
common used penetration enhancers, and we have two 
kinds of penetration enhancing effects of promotors 
studied. From this experiment, we can see that borneol 
and nitrogen mixed ketones showed the best penetration 
or transdermal promoting effects, indicating that borneol 
and Azone in the transdermal play a synergistic role in 
helping the drug penetrate the skin. Borneol alone and 
Azone alone, however, showed less transdermal effects. 
The role of borneol was stronger than Azone, suggesting 
a leading role of borneol and Azone as a supporting 
partner. Complicated ingredients of Chinese herbal 
compound, borneol partial fat-soluble and water-soluble 
Azone, the two combined is conducive to the overall 
absorption of active ingredients (Pan et al., 2006; Lin et
al., 2007).
 

 

https://drive.google...dit?usp=sharing

 

Borneol/Menthol used to increase flavonoid bioavailability 

 

 

 

 A borneol/menthol eutectic mixture has enhanced the brain transport of a drug when it was nasally coadministered with a polypeptide molecule (10). Daidzein (also called 4′,7-dihydroxylisoflavone) (Fig. 1), a water-insoluble isoflavone, is mainly present in leguminous plants, especially in soybeans, soy foods, and Pueraria lobata Ohwi (Leguminosae) (11,12). Daidzein can reduce breast cancer occurrence and also plays a key role in protecting against colon cancer (13). More recently, Wilcox and Blumenthal (14,15) have hypothesized that isoflavones may reduce the aggregation of platelets at the sites of arterial injury. These sites are associated with atherosclerotic development.

 

 

 

Compared with the daidzein suspension, the relative bioavailability of daidzein administered with borneol/menthol eutectic mixtures was 1.5-fold higher

 

http://www.ncbi.nlm....les/PMC3225554/

 

 

Ladies and gentlemen please stay tuned....



#9 medicineman

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Posted 27 July 2014 - 05:48 PM

the hallmark of ms and demyelination is bbb permeability (after damage) to leukocytes. you really want to make the only barrier between your brain and the rest of the world, more permeable?

#10 Metagene

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Posted 27 July 2014 - 06:42 PM

the hallmark of ms and demyelination is bbb permeability (after damage) to leukocytes. you really want to make the only barrier between your brain and the rest of the world, more permeable?

 

No not in a absolute sense. For instance Lysophosphatidic acid can be Co-administer with sphingosine-1-phosphate to quickly open and restore BBB integrity. This is still problematic because the procedure is invasive and LPA increase BACE1 expression and beta amyloid production . http://www.ncbi.nlm....pubmed/23036978

 

I posted a link in this thread on the BBB issue with nicotine. http://www.longecity...ootropic/page-2

 

Borneol could also raise blood concentration of some drugs to toxic levels (hence the lower dose of L-DOPA) so its a lot to consider.


Edited by Metagene, 27 July 2014 - 06:44 PM.

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#11 Metagene

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Posted 31 July 2014 - 05:58 PM

Update: I will have 25g of borneol at my disposal in a week or two. I want to procure a few more items to create a nasal solution as well.

#12 Metagene

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Posted 31 July 2014 - 09:03 PM

ETA on Borneol 1-3 days!

#13 Tom_

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Posted 04 August 2014 - 08:28 AM

Completely ignorant of the subject.

 

However, if you are actually planning on doing it...don't be a twat. The BBB is there to keep out pathogens and stop your brain getting bathed in a lot of shit its not able to deal with.

 

If its just theoretical - ah hell am I reading all of that but each to his own :)



#14 Metagene

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Posted 04 August 2014 - 02:37 PM

Completely ignorant of the subject.

 

However, if you are actually planning on doing it...don't be a twat. The BBB is there to keep out pathogens and stop your brain getting bathed in a lot of shit its not able to deal with.

 

If its just theoretical - ah hell am I reading all of that but each to his own :)

 

 

Your concern is much appreciated Tom_ but I'm sure I already fit that descriptor. Borneol does have antimicrobial and antibacterial properties so it maybe safer than other options. 

 


Edited by Metagene, 04 August 2014 - 02:38 PM.


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#15 Metagene

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Posted 14 August 2014 - 10:26 PM

It took longer than expected but my 25g of Borneol came today. I will try a little before bed with Baicalin.





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