Formulation of Ketoconazole Niosomal Delivery System using Non-Ionic Surfactants
Main Article Content
Abstract
Ketoconazole is a broad-spectrum Imidazole derivative antifungal that is effective for both superficial and systemic fungal infections that cannot be completely absorbed when administered orally because it has low solubility. This can be overcome by forming a ketoconazole niosome delivery system. Niosomes are vesicular systems formed using non-ionic surfactants that could increase the solubility and bioavailability of drugs. The purpose of this study was to form a ketoconazole niosome system to increase the bioavailability and therapeutic effectiveness of ketoconazole. Niosomes were made into nine formulas using 100 mg surfactant with variations in the combination of non-ionic surfactant concentrations Span 60 (70.80-98.29%):Sucrose Ester Palmitate (SEP) (1.71-29.20%), which produced Hydrophilic Liphophilic Balance (HLB) values between 4-8. The evaluations on niosomes were organoleptic tests, particle size tests, polydispersity indexes, zeta potentials, structural analysis using Forrier Transform Infra Red (FTIR), morphological analysis using Transmission Electron Microscope (TEM), entrapment efficiency tests and drug release tests. The results showed that the niosome system with an HLB value of 7.5 produced a vesicle size 336,13±3,14 nm, polydispersity index 0,000, zeta potensial -52,16±1,54 mV, spherical form of vesicle and no found chemistry interaction between the components (result of TEM and FTIR), an entrapment efficiency value of 87.86±0.18% and a drug release test value for 24 hours of 97.23±2.16%. This showed that the ketoconazole niosome system made using a combination of span 60 surfactants and SEP with an HLB value of 7.5 was able to produce an excellent niosome system.
Downloads
Article Details
This work is licensed under a Creative Commons Attribution-NonCommercial-NoDerivatives 4.0 International License.
How to Cite
References
Sodeifian G, Sajadian SA, Razmimanesh F, Hazaveie SM. Solubility of Ketoconazole (antifungal drug) in SC-CO2 for binary and ternary systems: measurements and empirical correlations. Sci Rep. 2021; 11(1).
Sipos E, Kósa N, Kazsoki A, Szabó ZI, Zelkó R. Formulation and characterization of Aceclofenac-loaded nanofiber based orally dissolving webs. Pharmaceutics. 2019; 11(8).
Mittal S, Chaudhary A, Chaudhary A, Kumar A. Proniosomes: The effective and efficient drug-carrier system. Ther Deliv. 2020; 11(2):125–137.
Chen S, Hanning S, Falconer J, Locke M, Wen J. Recent advances in non-ionic surfactant vesicles (niosomes): Fabrication, characterization, pharmaceutical and cosmetic applications. Eur J Pharm Biopharm. 2019; 144:18–39.
Govindarajan S, Swamivelmanickam M, Nair SP, Sivagnanam S. A comprehensive study on provesicular drug delivery system: Proniosomal gel. Indian J Pharm Sci. 2022; 84(1):1–13.
Theerdhala S, Harikrishnan N. Mupirocin loaded niosomal gel for topical wound healing applications. Trop J Nat Prod Res. 2023; 7(8):3676–3682.
Kumar GP, Rajeshwarrao P. Nonionic surfactant vesicular systems for effective drug delivery—an overview. Acta Pharm Sin B. 2011; 1(4):208–219.
Abu El-Enin AS, Khalifa MK, Dawaba A, Dawaba H. Proniosomal gel-mediated topical delivery of Fluconazole: Development, in vitro characterization, and microbiological evaluation. J Adv Pharm Technol Res. 2019; 10(1).
Rasul A, Khan MI, Rehman MU, Abbas G, Aslam N, Ahmad S, Abbas K, Akhtar Shah P, Iqbal M, Ahmed Al Subari AM, Shaheer T, Shah S. In vitro characterization and release studies of combined nonionic surfactant-based vesicles for the prolonged delivery of an immunosuppressant model drug. Int J Nanomedicine. 2020; 15:7937–7949.
Compass Food. Compass Food. 2023 [cited 2023 Dec 15]. Habo monoester P90. Available from: https://www.compassfoods.com/habo-monoester-p90.html
Shirsand S, Kanani K, Keerthy D, Nagendrakumar D, Para M. Formulation and evaluation of Ketoconazole niosomal gel drug delivery system. Int J Pharm Investig. 2012; 2(4).
Hariyanti, Damayanti S, Tarini S. Optimization process and characterization Cinchonine niosomes. Pharm J of Ind. 2019; 16(02):178–187.
De Silva L, Fu JY, Htar TT, Muniyandy S, Kasbollah A, Wan Kamal WHB, Chuah LH. Characterization, optimization, and in vitro evaluation of Technetium-99m-labeled niosomes. Int J Nanomedicine. 2019; 14:1101–1117.
Obeid MA, Khadra I, Aljabali AAA, Amawi H, Ferro VA. Characterisation of niosome nanoparticles prepared by microfluidic mixing for drug delivery. Int J Pharm X. 2022; 4.
Verma V, Singh UK. Ketoconazole HPLC Method development and validation: A novel approach. Int Res J of Pharm. 2017; 8(8):74–81.
Afreen U, Fahelelbom KM, Shah SNH, Ashames A, Almas U, Khan SA, Yameen MA, Nisar N, Hassan bin Asad MH, Murtaza G. Formulation and evaluation of niosomes-based chlorpheniramine gel for the treatment of mild to moderate skin allergy. J Exp Nanosci. 2022; 17(1):467–495.
Ugorji OL, Umeh ONC, Agubata CO, Adah D, Obitte NC, Chukwu A. The effect of niosome preparation methods in encapsulating 5-fluorouracil and real time cell assay against HCT-116 colon cancer cell line. Heliyon. 2022; 8(12).
Liga S, Paul C, Moacă EA, Péter F. Niosomes: Composition, formulation techniques, and recent progress as delivery systems in cancer therapy. Pharmaceutics. 2024; 16.
Owodeha-Ashaka K, Ilomuanya MO, Iyire A. Evaluation of sonication on stability-indicating properties of optimized pilocarpine hydrochloride-loaded niosomes in ocular drug delivery. Prog Biomater. 2021; 10(3):207–220.
Stoyanov Vassilev D, Petkova NT, Koleva M. Optimization of ultrasound synthesis of sucrose esters by selection of a suitable catalyst and reaction conditions. J of Chem Tech and Met. 2021; 56(2):268-274.
Indra I, Janah FM, Aryani R. enhancing the solubility of ketoconazole via pharmaceutical cocrystal. J. Phys: Conf. Series. 2019; 1179.
Sangkana S, Eawsakul K, Ongtanasup T, Boonhok R, Mitsuwan W, Chimplee S, Paul AK, Saravanabhavan SS, Mahboob T, Nawaz M, Pereira ML, Wilairatana P, Wiart C, Nissapatorn V. Preparation and evaluation of a niosomal delivery system containing G. mangostana extract and study of its anti-Acanthamoeba activity. Nanoscale Adv. 2024; 6(5):1467–1479.
Munandar R, Anam K, Hudiyanti D. The optimization of encapsulation Mangosteen (Garcinia mangostana L.)-Gotu Kola (Centella asiatica L. Urban) fraction combination in soybean liposome by response surface methodology. Trop J Nat Prod Res. 2023; 7(9):3944–3950.
Joshi S, White R, Sahu R, Dennis VA, Singh SR. Comprehensive screening of drug encapsulation and co-encapsulation into niosomes produced using a microfluidic Device. Processes. 2020; 8(5).
Yaghoobian M, Haeri A, Bolourchian N, Shahhosseni S, Dadashzadeh S. The impact of surfactant composition and surface charge of niosomes on the oral absorption of repaglinide as a BCS II model drug. Int J Nanomedicine. 2020; 15:8767–8781.
Witika BA, Bassey KE, Demana PH, Siwe-Noundou X, Poka MS. Current advances in specialised niosomal drug delivery: Manufacture, characterization and drug delivery applications. Int J Mol Sci. 2022; 23.