Innaxon

Ambroxol Lipodisq™ Sterile Solution

CHF 244.00
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IAX-700-108-L0011 mlCHF 244.00
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Product Details
Synonyms Trans-4-[[(2-amino-3,5-dibromophenyl)methyl]amino]; NA 872; Cyclohexanol
Product Type Chemical
Properties
Formula

C13H18Br2N2O . HCl

MW 378.1 . 36.5
CAS 23828-92-4
RTECS GV8423000
Purity Chemicals ≥95% (HPLC)
Appearance Colourless clear aqueous solution
Solubility Soluble in water, PBS, Tris and other physiological solutions as formulated in a proprietary, thermostable, aqueous lipid nanoparticulate formulation (Lipodisq).
Reconstitution Avoid the use of buffers with divalent ions such as Ca or Mg or pH <6.5 or >8.0, which can cause particle instability. Unformulated ambroxol is soluble in DMF, DMSO or ethanol .
Formulation Liquid, detergent-free discoidal nano-formulation made of styrene-maleic acid lipid particles (SMALP), lecithin and sterile water.
Concentration 1mg/ml (0.1% w/vol)
Biological Activity

Discoidal nano-particles can incorporate hydrophobic, poorly water-soluble compounds, such as lipids, lipoproteins and glycolipids. - Cell culture tested (human macrophage cell line) (MTT). - Recommended starting dilution: 1:200 or higher. - Optimal working concentrations depend on the applications and need to be determined. - Published procedures using Lipodisq formulations (Curcumin and IAXO TLR4 antagonists) in vivo rodent models at 3-10mg/kg. Recommended route of administration is subcutaneous (s.c.) with oral or nasal application as a possible alternative, which needs to be optimized.

Declaration Manufactured by Innaxon.
Other Product Data

Click here for Original Manufacturer Product Datasheet: Our product description may differ slightly from the original manufacturers product datasheet.


Lipodisq™ technology is covered by one or more of the following patents owned by Malvern Cosmeceutics Limited: AU2006253886, CA2611144, CN101184473B, EP1890675, GB2426703, IN261468, JP5142898, US8623414 and WO/2021/005340A1 pending. The purchaser is licensed under those patents to use these assemblies for the purpose of research and development only, but not for the purpose of delivery of agents for clinical use to humans or veterinary use to animals for therapeutic, diagnostic or prophylactic purposes, which uses are specifically prohibited.

InChi Key QNVKOSLOVOTXKF-PFWPSKEQSA-N
Smiles O[C@H]1CC[C@H](NCC2=CC(Br)=CC(Br)=C2N)CC1.Cl
Shipping and Handling
Shipping AMBIENT
Short Term Storage +4°C
Long Term Storage +4°C
Handling Advice Keep sterile.
Avoid skin and eye contact.
Use/Stability Stable for at least 1 year after receipt when stored at +4°C.
Documents
MSDS Inquire
Product Specification Sheet
Datasheet Download PDF
Description
  • Ambroxol Lipodisq Sterile Solution is a ready-to-use nano-formulated aqueous solution.
  • Ambroxol is a mucolytic agent used in the treatment of respiratory diseases. Ambroxol is a basic (pKa = 9.01) cationic drug with lipophilic properties (logP = 2.9), enabling it to act as a lysosomotropic agent. In addition, ambroxol exhibits a novel mechanism by accumulating in lamellar bodies and acting as a lysosomal secretagogue. A wide range of pharmacological effects of ambroxol has been confirmed, including mucus regulation, anti-inflammatory, reduction of arachidonic acid metabolites and pro-inflammatory cytokines, and antioxidant properties. In addition, ambroxol aids in the enhancement of local defense molecules involved in respiratory viral replication. Ambroxol is a sodium channel blocker and mucolytic agent with antioxidant, anti-viral and anti-inflammatory properties. Inhibits tetrodotoxin (TTX)-resistant channels more potently than TTX-sensitive subtypes. Inhibits the release of histamine, leukotrienes and cytokines from human leukocytes and mast cells. Inhibits viral replication and improves the survival rate of mice infected with influenza (H3N2) virus. It is a candidate for use as an anti-COVID19 therapeutic.
  • Ambroxol Lipodisq is based on a nanoparticle (11-40nm) drug delivery system comprising a discoidal phospholipid bilayer membrane stabilized by a chaperone molecule annulus. Internal properties of the phospholipid membrane support the disposition and stabilization of drug molecule candidates and preserve the native conformation of membrane molecules. The resulting encapsulated actives are rendered water-soluble and specialized for intra-cellular penetration/delivery via endosomal uptake mechanisms. Lipodisq solutions show a good safety profile and are suitable for in vitro and in vivo investigations.
Product References
  1. Ambroxol in the 21st century: pharmacological and clinical update: M. Malerba & B. Ragnoli; Expert Opin. Drug. Metab. Toxicol. 4, 1119 (2008) (Review)
  2. Ambroxol as a novel disease-modifying treatment for Parkinson’s disease dementia: protocol for a single centre, randomized, double-blind, placebo-controlled trial: C.R.A. Silveira, et al.; BMC Neurol. 19, 20 (2019)
  3. Azithromycin and ambroxol as potential pharmacotherapy for SARS-CoV-2: M. Alkotaji; Int. J.Antimicrob. Agents 56, 106192 (2020)
  4. Topical Treatments and Their Molecular/Cellular Mechanisms in Patients with Peripheral Neuropathic Pain-Narrative: M. Kocot-Kępska, et al.; Pharmaceutics 13, 450 (2021) (Review)
  5. Inhibition of acid sphingomyelinase by ambroxol prevents SARS-CoV-2 entry into epithelial cells: A. Carpinteiro, et al.; J. Biol. Chem. 296, 100701 (2021)

General References for Lipodisq™ Technology:


  1. Responsive Hydrophobically Associating Polymers: A Review of Structure and Properties: S.R. Tonge & B.J. Tighe; Adv. Drug Deliv. Rev. 53, 109 (2001)
  2. Detergent-free formation and physico-chemical characterization of nanosized lipidpolymer complexes: Lipodisq; M.C. Orwick, et al.; Angew. Chem. 51, 4653 (2012)
  3. Physicochemical Characterization, Toxicity and In Vivo Biodistribution Studies of a Discoidal, Lipid-Based Drug Delivery Vehicle: Lipodisq Nanoparticles Containing Doxorubicin: M.L. Torgersen, et al.; J. Biomed. Nanotechnol. 16, 41 (2020)
  4. Applications of Synthetic Polymer Discoidal Lipid Nanoparticles to Biomedical Research: M. Tanaka; Chem. Pharm. Bull. 70, 507 (2022)
  5. Mechanisms of Formation, Structure, and Dynamics of Lipoprotein Discs Stabilized by Amphiphilic Copolymers: A Comprehensive Review: P.S. Orekhov, et al.; Nanomaterials 12, 361 (2022)
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