Short Communication

Ebisilc® Organosilicate Particles for Innovative Galenic Formulation

Saddam Charaabi1,2, Pata-Eting Kougnassoukou Tchara1, Zouhair Bouaziz2, Christelle Marminon2, Gérard Holtzinger1, Anne-Marie Pensé-Lhéritier1, Marc Le Borgne2* and Samar Issa1*
1Department of Pharmacolgy, Ecole de Biologie Industrielle, France
2Department Pharmacie, Université de Lyon, France


*Corresponding author: Marc Le Borgne, Université Lyon, France


Published: 06 Nov, 2017
Cite this article as: Charaabi S, Kougnassoukou Tchara P-E, Bouaziz Z, Marminon C, Holtzinger G, Pensé-Lhéritier A-M. Ebisilc® Organosilicate Particles for Innovative Galenic Formulation. Ann Pharmacol Pharm. 2017; 2(20): 1103.

Short Communication

Clays, mineral clays and more interestingly organoclays [1] have been extensively described as complexation agents for drugs and bioorganic compounds.
Laboratory EBInnov® has developed a collection of novelorganosilicate particles synthesized by sol-gel procedure with a controlled ratio of hydrophobic/hydrophilic side chains [2]. Further investigations were carried out on the ability of these particles to stabilize Pickering emulsions [3]. From these customizable organ silicates with particular characteristics such as size distribution and Wettability, new organic-inorganic hybrid materials can be designed and synthesized.
Some studies described the complexation of UV-filters with various clay minerals of smectite group such as montmorillonites [4-6]. Therefore, in the first phase of a new project, a proof of concept study was carried out to combinelipophilic organ silicate particles with a UV filter and then to propose interesting innovation in the formulation of sunscreen emulsions. Then we started the complexation according to the works previously described by Ambrogi et al. [7] and Li et al. [8], using oxybenzone (BZ-3) as UV filter. We performed a large number of experiments involving the lipophilic organosilicateparticles SC002, Laponite® XLG (laponite) and natural white-pinkish montmorillonites Cos WHITE™ (MMT). Every complexation experiment with wet procedure required a clever choice of the solvent. In our case, the optimal solvent must dissolve the BZ-3 and easily disperse each of the three adsorbents (SC002, laponite, MMT) involved in the loading studies. Based on the Hansen solubility parameters, we performed a solubility card for a panel of solvents and UV filters using HSPiP 3.1 software as Benazzouz et al. [9] have reported for avobenzone. Then Hansen solubility parameters would predict the solubilization of solutes in solvents based on semiempirical description. Other parameters such as temperature and pH were also studied to rationalize our complexation [10]. A design-of-experiment approach to optimize actual data is performed and we will be able to propose new SC002-BZ-3 hybrids for sunscreen formulation, with expectation of a synergistic action toward photo stabilization.
In the second phase of our project, we are planning to involve other molecules in future complexation experiments, making SC002 particles as promising carriers of bioactive molecules. Then our studies should also include desorption experimentation to prove the reversible release of active pharmaceutical ingredients and their corresponding applications. Laboratory EA 4446 B2MC and his researchers have developed diverse small-molecule probes and drugs [11-18] and we will draw on their skills to design new bioactive molecules dedicated to be complexed with customizable organ silicates.


References

  1. Betega de Paiva L, Morales AR, Valenzuela Díaz FR. Organoclays: properties, preparation and applications. Appl Clay Sci. 2008;42(1-2):8-24.
  2. Lhéritier AM, Holtzinger G, Issa S, Rahali Y, Bensouda Y. inventors; Method for preparing clays having novel physico-chemical properties. EP2567940. 2013.
  3. Lorentz R, Rahali Y, Issa S, Bensouda Y, Holtzinger G, Aoussat A, et al. One-pot synthesis of sub-micron organosilicate particles for the formulations of Pickering emulsions. Powder Technol. 2014;264:446-57.
  4. Ogawa M, Ishii T, Miyamoto N, Kuroda K. Intercalation of a cationic azobenzene into montmorillonite. Appl Clay Sci. 2003;22(4):179-85.
  5. Paiva JP, Santos BAMC, Kibwila DM, Gonçalves TCW, Pinto AV, Rodrigues CR, et al. Titanium dioxide-montmorillonite nanocomposite as photoprotective agent against ultraviolet B radiation-induced mutagenesis in Saccharomyces cerevisiae: apotential candidate for safer sunscreens. J Pharm Sci. 2014;103(8):2539-45.
  6. Del Hoyo C, Vicente MA, Rives V. Preparation of drug-montmorillonite UV-radiation protection compounds by gas-solid adsorption. Clay Miner. 2001;36(4):541-6.
  7. Ambrogi V, Perioli L, Marmottini F, Latterini L, Rossi C, Costantino U. Mesoporous silicate MCM-41 containing organic ultraviolet ray absorbents: preparation, photostabilityand in vitro release. JPhysChem Solids. 2007;68(5-6):1173-7.
  8. Li CC, Lin YT, Chen YT, Sie SF, Chen-Yang YW. Improvement in UV protection retention capability and reduction in skin penetration of benzophenone-3 with mesoporous silica as drug carrier by encapsulation. J PhotochemPhotobiol B. 2015;148:277-83.
  9. Benazzouz A, Moity L, Pierlot C, Molinier V, Aubry J-M. Hansen approach versus COSMO-RS for predicting the solubility of an organic UV filter in cosmetic solvents. Colloids Surf A PhysicochemEng Asp. 2014;458:101-9.
  10. Issa S, KougnassoukouTchara PE, Holtzinger G, Davoust-Marminon C, Bouaziz Z, Le Borgne M, et al. Comparison of the complexation ability of natural clays and synthetic organosilicat with bioorganic compounds. 4th Congress on Innovation in Drug Delivery Site-Specific Drug, Antibes-Juan-les-Pins, France. 2016;P152.
  11. Le Borgne M, Marchand P, Le Baut G, Ahmadi M, Smith HJ, Nicholls PJ. Retinoic acid metabolism inhibition by 3-azolylmethyl-1H-indoles and 2, 3 or 5-(alpha-azolylbenzyl)-1H-indoles. J Enzyme Inhib Med Chem. 2003;18(2):155-8.
  12. Pagniez F, Abdala-Valencia H, Marchand P, Le Borgne M, Le Baut G, Robert-Piessard S, et al. Antileishmanial activities and mechanisms of action of indole-based azoles. J Enzyme InhibMed Chem. 2006;21(3):277-83.
  13. Lebouvier N, Pagniez F, Duflos M, Le Pape P, Na YM, Le Baut G, et al. Synthesis and antifungal activities of new fluconazole analogues with azaheterocycle moiety. Bioorg Med Chem Lett. 2007;17(13):3686-9.
  14. Bouaziz Z, Issa S, Gentili J, Gratz A, Bollacke A, Kassack M, et al. Biologically active carbazole derivatives: focus on oxazinocarbazoles and related compounds. J Enzyme Inhib Med Chem. 2015;30(2):180-8.
  15. Belhani B, Berredjem M, Le BorgneM, Bouaziz Z, Lebreton J, Aouf NE. A one-pot three-component synthesis of novel α-sulfamidophosphonates under ultrasound irradiation and catalyst-free conditions. RSC Adv. 2015;5(49):39324-9.
  16. Baiceanu E, Nguyen KA, Gonzalez-Lobato L, Nasr R, Baubichon-Cortay H, Loghin F, et al. 2-Indolylmethylenebenzofuranones as first effective inhibitors of ABCC2. Eur J Med Chem. 2016;122:408-418.
  17. Lamera E, Bouacida S, Le Borgne M, Bouaziz Z, Bouraiou A. Sequential MCR/Fisher indolization strategy for the facile construction of polycyclic carbazole derivatives. Tetrahedron Lett. 2017;58(13):1305-7.
  18. Bouzina A, Bechlem K, Becheker I, Belhani B, Berredjem H, Lebreton J, et al. Synthesis and in vitro antibacterial evaluation of novel functionalized sulfamidocarbonyloxyphosphonates. Molecules. 2017 .