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Determination of Histamine H -Receptor Antagonist Conessine In J Young Pharm, 2020; 12(1) : 55-62. A multifaceted peer reviewed journal in the field of Pharmacy Original Article www.jyoungpharm.org | www.phcog.net Determination of Histamine H3-Receptor Antagonist Conessine in Wistar Rat Plasma by a Rapid and Sensitive RP-UFLC Method: Application to a Pharmacokinetic Study Nilesh Sudhakar Ambhore1,*, Rama Satyanarayana Raju Kalidhindi1, Shubhashri Mohire2, Karthik Yamjala2, Shashank Mulukutla1, Vishakantha Murthy4, Mahesh Thondawada3, Kannan Elango1 1Department of Pharmacology, JSS College of Pharmacy, (JSS University, Ootacamund), Tamil Nadu, Ooty, INDIA. 2Department of Pharmaceutical Analysis, JSS College of Pharmacy, (JSS University, Ootacamund), Ooty, Tamil Nadu, INDIA. 3Department of Pharmaceutical Biotechnology, JSS College of Pharmacy, (JSS University, Ootacamund), Ooty, Tamil Nadu, INDIA. 4Molecular Pharmacology and Experimental Therapeutics, Mayo Clinic, Rochester, MN 55905, USA. ABSTRACT Objectives: Epidemiological data suggests the highest density of hista- mg/kg) administered orally to animals, demonstrated remarkable absorp- mine H3-receptors (H3R) in basal ganglia of central nervous system (CNS) tion into the systemic circulation with maximum concentration (~8700 ng/ wherein they function as inhibitory auto-receptors and control the release ml) within 2.0 h. The order of area under curve was found to be kidney> of many neurotransmitters. Inhibition of H3R increases the turnover of neu- brain> liver> lungs> spleen> heart. Conclusion: The liposomes of cones- rotransmitters, especially dopamine in basal ganglia and could be beneficial sine were rapidly taken up into the brain and showed a good brain concen- to treat Parkinson’s disease. Methods: In this study, we formulated the tration after 2.0 h; sustenance up to 4.0 h was achieved which is better brain targeting liposomes of conessine, a selective antagonist for H3R to than conessine solution. Key words: Conessine, RP-UFLC method, Pharmacokinetic, Tissue increase bioavailability and developed and validated a rapid and sensitive distribution, Validation. reverse phase ultra-force liquid chromatographic (RP-UFLC) method and to quantitate conessine in Wistar rat plasma and tissue. Plasma and tis- Correspondence sue samples were extracted by protein precipitation technique using ace- Dr. Nilesh S Ambhore, M.Pharm, Ph.D tonitrile (ACN) and aripiprazole as the internal standard. Chromatographic Department of Pharmacology, JSS College of Pharmacy, Rockland, Elkhill, Oo- separation was performed on the Hibar C column with a mobile phase 18 tacamund-643001, Ooty, Tamil Nadu, INDIA. of Hexane Sulphonic acid (10 mM, pH 10.0 adjusted with ammonia) and methanol at a flow rate of 0.9 ml/min.Results: The lower limit of quantifi- Phone: +91-9486016494 cation of the developed method was 4.0 ng/ml and 6.0 ng/g in plasma and Email: [email protected] tissue samples, respectively. Liposomes of conessine (equivalent to 20 DOI: 10.5530/jyp.2020.12.11 INTRODUCTION Parkinson’s disease (PD) is one of the commonly occurring neurodegen- mined. Thus, the etiology of PD remains difficult to establish leading to erative disorder which leads to muscular rigidity, bradykinesia, tremor challenges in development of clinical tools.13 1,2 of resting limbs and loss of postural balance. The main characteristic Histamine H3-receptor (H3R) were first discovered in 1983 as a pre- of PD involves degeneration of pigmented neurons in substantia nigra synaptic autoreceptors for the neurotransmitter histamine.14 A grow- 3,4 resulting in depletion of dopamine (DA) and its metabolites level. PD ing body of literature also supports a role for H3R in influencing the ranks among the most common late life neurodegenerative diseases, af- release of a number of additional neurotransmitters like acetylcholine fecting approximately 1.5-2.0 % of the population which is older than 60 (Ach), dopamine (DA), glutamate, noradrenaline (NA) and serotonin 14-16 years.5,6 Irrespective of enormous scientific research, exact physiological (5-HT). H3R are mainly located in cerebral cortex, hippocampus, causes of PD, the second most common neurodegenerative disorder, are amygdala, nucleus accumbens, globus pallidus, striatum and hypothala- 17,18 still largely unknown.7 Age is the single greatest risk factor for PD with mus; however, the highest density of H3R are found in basal ganglia, the number of world-wide cases increasing from an estimated 4.1 mil- an important seat in the brain involved in coordination of information from sensorimotor, motivational and cognitive brain areas to control be- lion (340,000 US cases) in 2005 to nearly 8.7 million (610,000 US cases) haviors such as movement and reward learning. The selective antagonist/ by 2030.8 inverse antagonist of H3R such as thioperamide (THP) and ciproxifan A subclinical phase exists prior to the appearance of Parkinsonism; dur- (CPX),19 potentiate neurochemical and behavioral effects of haloperidol 9,10 ing this period striatal compensatory phenomena, such as increased (HAL) and enhance the turnover of dopamine in midbrain of rats. Liter- neuronal activity or sensitization of dopaminergic receptors are acti- ature supports that it also modulates the neurochemical and behavioral vated.9,11 Therefore, PD is not clinically obvious before at least 50-70 % 20 effects of meth-amphetamine. This background suggests that H3R are of the dopaminergic neurons get degenerated. The first clinical signs are presynaptic auto-receptors which play an important role in modulating only observed when the degeneration is already strongly advanced.12 It various neurotransmitters in the mid brain. A specific antagonist or in- follows that the onset time point of the degeneration cannot be deter- verse agonist of H3R may thus increase the level of dopamine in mid This is an open access article distributed under the terms of the Creative Commons Attribution-NonCommercial-ShareAlike 4.0 License, which allows others to remix, tweak, and build upon the work non-commercially, as long as the author is credited and the new creations are licensed under the identical terms. Journal of Young Pharmacists, Vol 12, Issue 1, Jan-Mar, 2020 55 Ambhore, et al.: Estimation of Conessine using Simple and Sensitive RP-UFLC Method in Rat Plasma brain and prove to be effective to treat Parkinsonism and other neurode- Tissue preparation generative diseases. After treatment regimen, animals were sacrificed and blood was collect- Conessine is a steroidal alkaloid found in a number of plant species from ed by cardiac puncture method into 4 ml tubes pretreated with sodium 21 the Apocynaceae family, including Holarrhena floribunda, Halorrhena heparin (68 USP units) anticoagulant. The important vital organs (brain, 22 23 antidysenterica and Funtumia elastica. It is one of the potent and se- liver, lungs, kidney, spleen and heart) were quickly removed and stored 24 lective H3R subtype antagonist. It is well proven that conessine, an H3R at -70 ± 2°C until analysis. For estimation, tissue samples were weighed antagonist exacerbated ethanol-induced psychostimulation by altering accurately and homogenized using a glass tissue homogenizer after addi- 25 dopaminergic neurotransmission in the nigrostriatal pathway. To the tion of Tris KCl buffer (10 mM pH 7.4); homogenised organs and blood best of our knowledge, there are no detailed reports on the pharmacoki- were centrifuged at 10,500 X g for 20 min to obtain a clear supernatant netic and tissue distribution properties of conessine using revers phase and plasma.27,28 ultra-fast liquid chromatographic (RP-UFLC). Therefore, this study aimed to develop and validate a highly selective and sensitive method Extraction of plasma and tissue samples based on RP-UFLC for routine analysis of conessine in rat plasma. Also, A 500 µl of plasma, 500 µl of IS (100 µg/ml) and 500 µl of ACN were we aimed to investigate the pharmacokinetics and tissue distribution aliquoted into 2 ml eppendorf tube, vortexed for 30s then centrifuged profile of conessine in Wistar rats after oral administration at 20 mg/kg; (Remi Instruments, Mumbai) at 10,000 rpm for 10 min. The clear su- the said dose having been established in ischemic renal injury in Wistar pernatant solution was transferred into a vial and 20 µl was injected to rats.26 UFLC analysis. Similarly, tissue homogenates were processed and ana- MATERIALS AND METHODS lyzed by UFLC. Chemicals and reagents Method validation Conessine ≥97 % (HPLC) and Aripiprazole were obtained from Sigma- The UFLC method to determine biodistribution of conessine in Wistar Aldrich (St. Louis USA). The chemical structure of conessine and aripip- rat plasma and tissue was validated as per the USFDA guidelines.29,30 The razole are shown in Figure 1. The HPLC grade methanol and acetoni- method of determination was validated for specificity, extraction recov- trile were purchased from SD Fine chemicals (Mumbai, India); Hexane ery, linearity, sensitivity, accuracy, precision and stability. Sulphonic acid, Trisaminomethane (TRIS), sodium chloride, Potassium Specificity: is the ability of an analytical method to differentiate and chloride, ammonium solution and potassium dihydrogen phosphate quantify the analyte in the presence of other components in the sample. of AR grade were procured from SD Fine chemicals (Mumbai, India). The specificity was ascertained by the lack of interference peaks at the Ortho-phosphoric acid and di-methyl sulphoxide (DMSO) of AR grade retention time of conessine and the aripiprazole (internal standard). The
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