Solubilization of Insoluble and Poorly-Water Soluble Drugs in Micellar Systems
Abstract views: 181 / PDF downloads: 52
DOI:
https://doi.org/10.62482/pmj.9Anahtar Kelimeler:
Surfactant, poorly soluble drugs, critical micelle concentration, micelle, solubilizationÖzet
Introduction: This study investigates the micellar solubilization of several insoluble and poorly soluble drugs—clopidogrel bisulfate, ganciclovir sodium, miconazole nitrate, brinzolamide, brimonidine tartarate, and dexamethasone—using sodium dodecyl sulfate (SDS), aerosol-OT (AOT), dodecyl trimethylammonium bromide (DTAB), and cetyltrimethylammonium bromide (CTAB) as surfactants.
Methods: The micellar solubilization experiments were conducted by preparing solutions of the drugs in the presence of SDS, AOT, DTAB, and CTAB micelles. Spectrophotometric measurements were performed at a constant temperature of 298 K to analyze the solubilization efficiency of each surfactant. Phase-solubilization graphs were plotted to visualize the relationship between drug solubility and surfactant concentration.
Results: The results indicated that hydrophobic interactions play a critical role in surfactant solubilization power. AOT was identified as the most effective surfactant among those tested. The solubility tendencies of the drugs in the presence of micelles were discussed based on the calculated KM values and the spectral behavior of drug molecules.
Conclusion: Micellar solubilization offers a promising approach to characterize drugs with varying solubility profiles—ranging from slightly soluble to insoluble in water. Additionally, surfactant micelles serve as effective biomimetic models for membrane systems in pharmaceutical research. the findings from this study hold implications for drug formulation and design, particularly in addressing solubilization challenges and optimizing pharmaceutical dosage forms.
Referanslar
Elworthy PH, Florence AT, Macfarlene CB. Solubilization by surface-active agents. Chapman and Hall Ltd; USA, 1968.
Florence AT, Attwood D. Physicochemical principles of pharmacy. 3rd ed. The MacMillan Press; London, 2003.
Rosen MJ. Surfactants and interfacial phenomena. 2ed. John Wiley & Sons; New York, 1989.
Sweetana S, Akers MJ. Solubility principles and practices for parenteral drug dosage form development. PDA J Pharm Sci Technol. 1996; 50 (5):330–342.
Rangel-Yagui CO, Pessoa A Jr, Tavares LC. Micellar solubilization of drugs. J Pharm Pharm Sci. 2005;8(2):147-165.
Ullah I, Baloch M K, Durrani GF. Solubility of nonsteroidal anti-inflammatory drugs (NSAIDs) in aqueous solutions of non-ionic surfactants. J Solut Chem. 2011; 40 (7)1341–1348. https://doi.org/10.1007/s10953-011-9709-z
Corrigan OI, Healy AM. Surfactants in pharmaceutical products and systems, in Encyclopedia of Pharmaceutical Technology, J. Swarbrick and J. C. Baylan, Eds., pp. 2639–2653, Marcel Dekker; New York, NY, USA, 2002.
Gokturk S, Caliskan E, Talman RY, Var U. A study on solubilization of poorly soluble drugs by cyclodextrins and micelles: complexation and binding characteristics of sulfamethoxazole and trimethoprim. ScientificWorldJournal. 2012; https://doi.org/10.1100/2012/718791.
Gokturk S, Aslan S. Study on binding properties of poorly soluble drug trimethoprim in anionic micellar solutions. J Dispers Sci Technol. 2014; 35: 84-92. https://doi.org/10.1080/01932691.2013.775583
Göktürk S. Tamer ZB. Interactions and solubilization of poorly soluble drugs in aerosol-OT micelles. J Surfactants Deterg. 2018;(21): 889-898. https://doi.org/10.1002/jsde.12192
Kawakami K, Miyoshi K, Ida Y. Solubilization behavior of poorly soluble drugs with combined use of Gelucire 44/14 and cosolvent. J Pharm Sci. 2004; 93: 1471–79. https://doi.org/10.1002/jps.20067
Park SH, Choi HK. The effects of surfactants on the dissolution profiles of poorly water-soluble acidic drugs. Int J Pharm. 2006;(321): 35-41. https://doi.org/10.1016/j.ijpharm.2006.05.004
Maswal M, Chat OA, Jabeen S, Ashraf U, Masrat R, Shah RA, Dar AA. Solubilization and co-solubilization of carbamazepine and nifedipine in mixed micellar systems: insights from surface tension, electronic absorption, fluorescence and HPLC measurements. Rsc Advances. 2015; (5): 7697-7712. https://doi.org/10.1039/C4RA09870F
Hanif S, Usman M, Hussain A, Rasool N, Khan A, Jamal MA, Elgorban AM, Ali Rana U. Spectroscopic study of benzothiophene partitioning in sodium dodecyl sulfate and cetyl trimethyl ammonium bromide micellar media. J Surfact Deterg. 2016; 19:1033–1041. https://doi.org/10.1007/s11743-016-1852-1855
Higuchi TA, Connors KA. Phase-solubility techniques. In: C. N. Reilly, Ed.,Advances in Analytical Chemistry and Instrumentation, Wiley-Interscience, 4, 117-122 :1965.
Yang G, Jain N, Yalkowsky SH. Combined effect of SLS and (SBE)7M-β-CD on the solubilization of NSC-639829. Int J Pharm. 2004; (269): 141–148. https://doi.org/10.1016/j.ijpharm.2003.09.001
Wang Z, Burrell LS, Lambert W.J. Solubility of E2050 at various pH: A Case in which apparent solubility is affected by the amount of excess solid. J Pharm Sci. 2002; (91); 1445-1455. https://doi.org/10.1002/jps.10107
Göktürk S, Var U. Effect of pharmaceutically important cosolvents on the interaction of promethazine and trifluopromazine hydrochloride with sodium dodecyl sulfate micelles. J Dispers Sci Technol. 2012; (33): 527-535. https://doi.org/10.1080/01932691.2011.574934
İndir
Yayınlanmış
Nasıl Atıf Yapılır
Sayı
Bölüm
Lisans
Telif Hakkı (c) 2024 Pharmedicine Journal
Bu çalışma Creative Commons Attribution 4.0 International License ile lisanslanmıştır.