Formulation and in vitro /in vivo Evaluation of Silymarin Solid Dispersion- Based Topical Gel for Wound Healing
DOI:
https://doi.org/10.31351/vol32issSuppl.pp42-53Keywords:
silymarin , solid dispersion , nicotinamide, wound healing, topical gelAbstract
Silybum marianum, from which silymarin (SM) is extracted, is a medicinal herb. In the Biopharmaceutics Classification System, it is of the class II type, meaning it is almost completely insoluble in water. It has a number of therapeutic properties, including anti-inflammatory as well as properties that promote wound healing.
This research target is to promote the dissolution and solubility of SM by employing a technique called solid dispersion and then incorporating the formula of solid dispersion into a topical gel that can be used for wound healing.
Solid dispersion is a technique used to enhance solubility and dissolve pharmaceuticals that are not water-soluble. This method is widely used because of its low cost and high efficiency. Because of its capacity to repair skin, the hydrophilic carrier nicotinamide (NA) was selected in this investigation as the carrier. Kneading, solvent evaporation and fusion with a consistent drug-to-carrier ratio were the three separate processes utilized in the preparation of solid dispersion (1:1, 1:3, and 1:5). In addition, the products were examined to determine their physical characteristics and the degree of crystallinity. The selected formula was combined into a hyaluronic acid base gel using the cold method. This gel was then evaluated in vitro for physical qualities and put to an in vivo (animal) examination to determine how it healed wounds.
The study found that the solvent evaporation made SM 25 times more soluble and caused all of it to be released in 20 minutes for a 1:3 ratio.
Additional research using DSC and XRD demonstrated the amorphous nature of the result. According to FTIR, there was no evidence of interaction between the two.
The gel formula had good qualities, like a pH of 6.6, good spreadability, and drug release within three hours. It also contributed to the rapid healing of wounds.
How to Cite
Publication Dates
References
Soleimani V, Delghandi PS, Moallem SA, Karimi G. Safety and toxicity of silymarin, the major constituent of milk thistle extract: An updated review. Phytotherapy Research. 2019;33(6):1627–38.
Ferraz AC, Almeida LT, da Silva Caetano CC, da Silva Menegatto MB, Souza Lima RL, de Senna JPN, et al. Hepatoprotective, antioxidant, anti-inflammatory, and antiviral activities of silymarin against mayaro virus infection. Antiviral Res. 2021;194 :105168.
Tabari SA, Carpi S, Polini B, Nieri P, Esfahani ML, Moghadamnia AA, et al. Topical application of silymarin enhances cutaneous wound healing in rats. South African Journal of Botany . 2019;124:494–8.
di Costanzo A, Angelico R. Formulation strategies for enhancing the bioavailability of silymarin: The state of the art. Molecules. 2019;24(11):1–29.
Bhalani D v., Nutan B, Kumar A, Singh Chandel AK. Bioavailability enhancement techniques for poorly aqueous soluble drugs and therapeutics. Biomedicines. 23;10(9):2055.
Bhuyan C, Saha D, Rabha B. A brief review on topical gels as drug delivery system. J Pharm Res Int. 2021;33:344–57.
R. Jadhav K, Y. Pawar A, S. Sanap A, P. Rathod S, S. Malpure P, S. Bachhav R. Design and characterization of fluconazole loaded nanosponges containing topical gel preparation. Int J Life Sci Pharma Res. 2022;12(5):85–98.
Ghareeb MM, Abdulrasool AA, Hussein AA, Noordin MI. Kneading technique for preparation
of binary solid dispersion of meloxicam with poloxamer 188. 2009;10(4):1206–15.
Trasi NS, Bhujbal S v., Zemlyanov DY, Zhou Q (Tony), Taylor LS. Physical stability and release properties of lumefantrine amorphous solid dispersion granules prepared by a simple solvent evaporation approach. Int J Pharm X 2020;2(January):100052. 2590-1567 .
Agafonov M, Ivanov S, Terekhova I. Improvement of pharmacologically relevant properties of methotrexate by solid dispersion with Pluronic F127. Materials Science and Engineering C . 2021;124:112059.928-4931
Rupal J, Kaushal J, Mallikarjuna SC, Dipti P. Preparation and evaluation of topical gel of valdecoxib. International Journal of Pharmaceutical Sciences and Drug Research. 2010; 2(1): 51-54
Kassab HJ, Thomas LM, Jabir SA. Development and physical characterization of a periodontal bioadhesive gel of gatifloxacin. International Journal of Applied Pharmaceutics. 2017;9(3):31-36.
Alwossabi AM, Elamin ES, Ahmed EMM, Abdelrahman M. Solubility enhancement of some poorly soluble drugs by solid dispersion using Ziziphus spina-christi gum polymer. Saudi Pharmaceutical Journal. 2022 1;30(6):711–25.
Yang G, Zhao Y, Feng N, Zhang Y, Liu Y, Dang B. Improved dissolution and bioavailability of silymarin delivered by a solid dispersion prepared using supercritical fluids. Asian J Pharm Sci . 2015;10(3):194–202.
Inam S, Irfan M, Lali NUA, Syed HK, Asghar S, Khan IU, et al. Development and characterization of Eudragit® EPO-Based solid dispersion of rosuvastatin calcium to foresee the impact on solubility, dissolution and antihyperlipidemic Activity. Pharmaceuticals. 2022;15(4).492.
Suvidha Suryakant Patil, Shriniwas Krishna Mohite. Development and evaluation of solid dispersion incorporated topical gel of Nabumetone. Research J. Pharm. and Tech. 2014; 7(12):1413-1419.
Lobo MS, Costa P. Modeling and comparison of dissolution profiles ´. 2001;13:123–33.
Tekko IA. Polyethylene Glycol-based solid dispersions to enhance eprosartan mesylate dissolution and bioavailability. Archives of Pharmacy & Pharmacology Research. 2019;2(3):1–11.
Patel VP, Patel AP, Shah A. Optimization of amorphous solid dispersion techniques to enhance solubility of febuxostat. Folia Med (Plovdiv). 2021;63(4):557–68.
Aldawsari MF, Anwer MK, Ahmed MM, Fatima F, Soliman GA, Bhatia S, et al. Enhanced dissolution of sildenafil citrate using solid dispersion with hydrophilic polymers: Physicochemical characterization and in vivo sexual behavior studies in male rats. Polymers (Basel). 2021;13(20):1–15.
Elfakhri KH, Niu M, Ghosh P, Ramezanli T, Raney SG, Ahmed S, et al. Physicochemical and structural evaluation of microparticles in tretinoin topical gels. Int J Pharm. 2022 May 25;620:121748.
Nurman S, Yulia R, Irmayanti, Noor E, Sunarti TC. The optimization of gel preparations using the active compounds of arabica coffee ground nanoparticles. Sci Pharm. 2019;87(4).
Sadeq ZA, Sabri LA, Al-Kinani KK. Natural polymer Effect on gelation and rheology of ketotifen-loaded pH-sensitive in situ ocular gel (Carbapol). Journal of Advanced Pharmacy Education and Research. 2022;12(2):45–50.
Sampatrao KA, Bhalchandra KJ, Ravindra J, Manohar P. Formulation development and evaluation of Silymarin gel. Res J Pharm Technol. 2011;4(10):1633–6.
Jabbar SS, Najim SM, Fadhil AA. Evaluation of anti-inflammatory activities of newly synthesized isatin derivatives in rats. International Research Journal Of Pharmacy. 2019;10(2):75–80.
Ehrlich HP, Hunt TK. The effects of cortisone and anabolic steroids on the tensile strength of healing wounds. Ann Surg. 1969;170(2):203–6.
Dispersions S. Effect of hydrophilic carriers for solubility and dissolution enhancement of effect of hydrophilic carriers for solubility and dissolution enhancement of Sulfamerazine by solid dispersions technique. 2021;(December).
Ismail MY, M. Ghareeb M. Enhancement of the solubility and dissolution rate of Rebamipide by using solid dispersion technique (Part I). Iraqi Journal of Pharmaceutical Sciences . 2018;27(2):55–65.
Michael E. Aulton KMGT. Aulton-Pharmaceutics-The-design-and-manufacture-of-medicines-5th-Edition. Vol. 5, Aulton’s Pharmaceutics The Design and Manufacture of Medicines. 2018. 933 p.
Cardot JM, Garcia Arieta A, Paixao P, Tasevska I, Davit B. Implementing the biopharmaceutics classification system in drug development: reconciling similarities, differences, and shared challenges in the EMA and US-FDA-recommended approaches. AAPS Journal . 2016;18(4):1039–46.
Effect GP, Type C, Mohylyuk V, Pauly T, Dobrovolnyi O, Scott N, et al. Effect of carrier type and tween ® 80 concentration on the release of Silymarin from amorphous solid dispersions. J Drug Deliv Sci Technol . 2021 Jun 1;63:102416.
Ali AMA, Al-Remawi MMA. Freeze dried quetiapine-Nicotinamide binary solid dispersions: A new strategy for improving physicochemical properties and ex vivo diffusion. J Pharm (Cairo). 2016;2016:1–11.
Choi MJ, Woo MR, Choi HG, Jin SG. Effects of polymers on the drug solubility and dissolution enhancement of poorly water-soluble Rivaroxaban. Int J Mol Sci. 2022;23(16).
Song I-S, Nam S-J, Jeon J-H, Park S-J, Choi M-K. Enhanced bioavailability and efficacy of Silymarin solid dispersion in rats with Acetaminophen-induced hepatotoxicity. Pharmaceutics. 2021; 13(5):628.
Ala’A DN, Al-Khedairy EBH. Formulation and evaluation of silymarin as microcrystals by in- Situ micronization technique. Iraqi Journal of Pharmaceutical Sciences. 2019;28(1):1–16.
Downloads
Published
Issue
Section
License
Copyright (c) 2023 Iraqi Journal of Pharmaceutical Sciences ( P-ISSN 1683 - 3597 E-ISSN 2521 - 3512)
This work is licensed under a Creative Commons Attribution 4.0 International License.
