Formulation, Evaluation, And Optimization of Coscinium Fenestratum-Based Niosomal In-Situ Gel for Anti-Cataract
Pharmaceutical Science-Pharmaceutics
DOI:
https://doi.org/10.22376/ijlpr.2023.13.4.P14-P28Keywords:
Cataract, Niosomes, In-situ gel, Coscinium fenestratum, GelAbstract
Coscinium fenestratum is a sturdy, creeping, woody plant that grows with a cylindrical, yellowish stem that belongs to the family Menispermaceae and is commonly known as tree turmeric. The research aims to develop a niosomal in-situ gel by incorporating a novel drug carrier, such as a niosome containing herbal extract for treating cataracts. The niosomal carrier was prepared by varying concentrations of two surfactants, while the herbal drug and cholesterol concentration was kept constant. The optimization of the niosome was done based on the size and shape of the vesicle obtained from SEM analysis. The optimized niosomal dispersion was then converted to a niosomal in-situ gel, and evaluations were carried out, like pH, viscosity, gelling capacity, gel strength, and isotonicity. From the preliminary phytochemical screenings of Coscinium fenestratum, the ethanolic extract showed the intense presence of flavonoids, alkaloids, steroids, and saponins. The drug-loaded niosomes were stable in HPMC, HPMC K15M, and Carbopol 940 ocular in-situ Gel, and the optimum HLB value of the surfactant span 60 made this formulation more stable. The Brookfield viscometer determined the viscosity, which is an important factor in determining the residence time of the drug in the eye. It possessed good viscosity of about 982.66 ± 1.52 cps. From a gelling capacity study conducted, it was found that the niosomal in-situ Gel possesses immediate gelation and remains for an extended period. The gel strength of niosomal in-situ Gel was 1.30 ± 0.006 sec, and when subjected to isotonicity testing, the results were acceptable. Stability studies were conducted at two different temperatures where no color changes occurred, and there was not much difference in parameters like pH, viscosity, gelling capacity, and gel strength. So it was concluded that the niosomal in-situ Gel of Coscinium fenestratum can be an alternative method to reduce the drawbacks of conventional ophthalmic dosage forms.
References
Pathak K, Das RJ, Herbal Medicine A. Rational approach in the health care system. Int J Herb Med. 2013:1-4.
Bhokare SG, Dongaonkar CC, v Lahane S, et al. Herbal novel drug delivery – a review. World J Pharm Pharm Sci. 2016;5:593-611.
Patel DK, Prasad SK, Kumar R, Hemalatha S. Cataract: A major secondary complication of diabetes, its epidemiology and an overview on major medicinal plants screened for anticataract activity. Asian Pac J Trop Dis. 2011;1(4):323-9. doi: 10.1016/S2222-1808(11)60075-3.
Shichi H. Cataract formation and prevention. Expert Opin Investig Drugs. 2004;13(6):691-701. doi: 10.1517/13543784.13.6.691, PMID 15174955.
Ahmed K, Gupta R, Gupta B. Cataract research in India: A scientometric study of publications output, 2002-2011. Int J Med Public Health. 2014;4(4):311-5. doi: 10.4103/2230-8598.144054.
Abdelkader H, Alany RG, Pierscionek B. Age-related cataract and drug therapy: opportunities and challenges for topical antioxidant delivery to the lens. J Pharm Pharmacol. 2015;67(4):537-50. doi: 10.1111/jphp.12355, PMID 25643848.
Nartey A. The pathophysiology of cataract and major interventions to retarding its progression: A mini-review, advances in ophthalmology & visual system. 2017;6:2-6.
Saso L, Silvestrini B. Antidenaturant drugs for cataract and other condensation diseases. Med Hypotheses. 2001;56(1):114-20. doi: 10.1054/mehy.2000.1128, PMID 11133267.
Liu YC, Wilkins M, Kim T, Malyugin B, Mehta JS. Cataracts. Lancet. 2017;390(10094):600-12. doi: 10.1016/S0140-6736(17)30544-5, PMID 28242111.
Alshamrani AZ. Cataracts pathophysiology and management. Egypt J Hosp Med. 2018;70(1):151-4. doi: 10.12816/0042978.
Takahashi Y, Fukusato T, Chapter 13. Animal models of liver diseases, animal models for studying human disease. 2nd ed. Vol. 45; 2017. p. 313-39.
Khan Mohd G, Novel Drug T-T. Delivery system. World J Pharm Pharm Sci. 2017:477-87.
Kute PR, Gondkar SB, Saudagar RB. Ophthalmic in-situ gel: an overview. World J Pharm Pharm Sci. 2015;4:549-68.
Dabir PD, Shahi SR, Deore SV. Ophthalmic in situ Gel: a review, European. J Pharm Med Res. 2016;3:205-15.
Thirumalai D, Paridhavi M, Gowtham M. Evaluation of physiochemical, pharmacognostic and phytochemical parameters of Premna herbacea. Asian J Pharm Clin Res. 2013;6(1):173-81.
Manokari DSL. A Study on the Extraction Process of Wrightia Tinctoria and Evaluation of Its Antimicrobial Activity. IJRASET;V():1308-16. doi: 10.22214/ijraset.2017.9188.
Gowtham M, Asharani IV, Thirumalai D. Determination of physiochemical, pharmacognostic, and phytochemical parameters of Premna herbacea. Technological innovation in pharmaceutical research. 2021;6:88-104.
Punitha ISR, Rajendran K, Shirwaikar A, Shirwaikar A. Alcoholic stem extract of Coscinium fenestratum regulates carbohydrate metabolism and improves antioxidant status in streptozotocin-nicotinamide induced diabetic rats. Evid Based Complement Alternat Med. 2005;2(3):375-81. doi: 10.1093/ecam/neh099, PMID 16136216.
Madhavan SC, Mathew TP. Indian medicinal plant, Coscinium fenestratum-A new bio Source for the multifunctional bioactive molecule–ecdysterone. Int J Herb Med. 2014;2:5-9.
Kar K, Sudheer P. Formulation and evaluation of niosomal drug delivery system of ketoprofen, RGUHS. J Pharm Sci. 2015;5:173-80.
Shirsand SB, Kumar GR, Keshavshetti GG, et al. Formulation and evaluation of clotrimazole niosomal gel for topical application, RGUHS. J Pharm Sci. 2015;5:32-8.
Patel KK, Kumar P, Thakkar HP. Formulation of niosomal Gel for enhanced transdermal lopinavir delivery and its comparative evaluation with autosomal Gel. AAPS PharmSciTech. 2012;13(4):1502-10. doi: 10.1208/s12249-012-9871-7, PMID 23104306.
El-Menshawe SF, Hussein AK. Formulation and evaluation of meloxicam niosomes as vesicular carriers for enhanced skin delivery. Pharm Dev Technol. 2013;18(4):779-86. doi: 10.3109/10837450.2011.598166, PMID 21913880.
Nadzir MM, Fen TW, Mohamed AR, et al. Size and stability of curcumin niosomes from combinations of Tween 80 and span 80. Sains Malays. 2020;46:2455-60.
De Leo V, Milano F, Mancini E, Comparelli R, Giotta L, Nacci A, et al. Encapsulation of curcumin-loaded liposomes for colonic drug Delivery in a pH-responsive polymer cluster using a pH-driven and organic solvent-free process. Molecules. 2018;23(4):739. doi: 10.3390/molecules23040739, PMID 29570636.
Kazi KM, Mandal AS, Biswas N, Guha A, Chatterjee S, Behera M, et al. Niosome: A future of targeted drug delivery systems. J Adv Pharm Technol Res. 2010;1(4):374-80. doi: 10.4103/0110-5558.76435, PMID 22247876.
Shilakari Asthana G, Asthana A, Singh D, Sharma PK. Etodolac Containing Topical Niosomal Gel: Formulation Development and Evaluation. J Drug Deliv. 2016;2016:9324567. doi: 10.1155/2016/9324567, PMID 27478643.
Jaiswal P. Gujarathi DrNA, formulation of niosomal Gel of diclofenac sodium and its in vitro characterization; 2016. p. 545-9.
Irshad Md, Zafaryab Md, Singh M, Rizvi MM. Comparative Analysis of the Antioxidant Activity of Cassia fistula Extracts. Int J Med Chem. 2012;2012:157125. doi: 10.1155/2012/157125, PMID 25374682.
Mariam Joshua J, Anilkumar A, Cu V, T Vasudevan D, A Surendran S. Formulation and evaluation of antiaging phytosomal Gel. Asian J Pharm Clin Res. 2018;11(3):409-23. doi: 10.22159/ajpcr.2018.v11i3.24257.
Bernatoniene J, Masteikova R, Davalgiene J, et al. Topical application of Calendula officinalis (L.): formulation and evaluation of hydrophilic cream with antioxidant activity. J Med Plants Res. 2011;5:868-77.
Ali HSM, Hanafy AF. Glibenclamide nanocrystals in a biodegradable chitosan patch for transdermal delivery: engineering, formulation, and evaluation. J Pharm Sci. 2017;106(1):402-10. doi: 10.1016/j.xphs.2016.10.010, PMID 27866687.
Shaikh A, Farheen T, Shahi S. pH triggered in-situ Gel: formulation development and evaluation of in situ ophthalmic Gel of olopatadine hydrochloride. Int J Pharm Sci Rev Res. 2015;35:180-5.
Waghulde V, Saudagar R. Formulation development and evaluation of Ph triggered in situ ophthalmic Gel of Besifloxacin hydrochloride. J Drug Delivery Ther. 2018;8(5):313-21. doi: 10.22270/jddt.v8i5.1874.
Nanjwade BK, Manjappa AS, Murthy RSR, et al. A novel was pH-triggered in situ gel for Sustained ophthalmic delivery of ketorolac tromethamine. Asian J Pharm Sci. 2009;4:189-99.
Nostro A, Germanò MP, D’Angelo V, Marino A, Cannatelli MA. Extraction methods and bioautography for evaluation of medicinal plant antimicrobial activity. Lett Appl Microbiol. 2000;30(5):379-84. doi: 10.1046/j.1472-765x.2000.00731.x, PMID 10792667.
Mukherjee PK. Quality control of herbal drugs. 1st ed. Pharmaceutical Press; 2002.
Tempone AG, Borborema SET, de Andrade Jr HF, de Amorim Gualda NC, Yogi A, Carvalho CS, et al. Antiprotozoal activity of Brazilian plant extracts from isoquinoline alkaloid-producing families. Phytomedicine. 2005;12(5):382-90. doi: 10.1016/j.phymed.2003.10.007, PMID 15957374.
Erdemoglu N, Ozkan S, Tosun F. Alkaloid profile and antimicrobial activity of Lupinus angustifolius L. alkaloid extract. Phytochem Rev. 2007;6(1):197-201. doi: 10.1007/s11101-006-9055-8.
El-Menshawe SF, Hussein AK. Formulation and evaluation of meloxicam niosomes as vesicular carriers for enhanced skin delivery. Pharm Dev Technol. 2013 Jul-Aug;18(4):779-86. doi: 10.3109/10837450.2011.598166, PMID 21913880.
Nair AS, Vidhya KM, Saranya TR, Sreelakshmy KR, Nair SC. Mucoadhesive buccal patch of cefixime trihydrate using biodegradable natural polymer. Int J Pharm Pharm Sci. 2014;6(6):366-71.
Teaima MH, Abdelhalim SA, El-Nabarawi MA, Attia DA, Helal DA. Non-ionic surfactant-based vesicular drug delivery system for topical caffeine delivery for cellulite treatment: design, formulation, characterization, histological anti-cellulite activity, and pharmacokinetic evaluation. Drug Dev Ind Pharm. 2018;44(1):158-71. doi: 10.1080/03639045.2017.1386206, PMID 28956468.
Jyoti K, Pandey RS, Madan J, et al. Inhalable cationic nio-somes of curcumin enhanced drug delivery and apoptosis in lung cancer cells. Indian J Pharm Educ Res. 2017;50;Suppl 21:S31.
Okore VC, Attama AA, Ofokansi KC, Esimone CO, Onuigbo EB. Formulation and evaluation of niosomes. Indian J Pharm Sci. 2011 May;73(3):323-8. doi: 10.4103/0250-474X.93515, PMID 22457561.
Shahiwala A, Misra A. Studies in topical application of niosomally entrapped nimesulide. J Pharm Pharm Sci. 2002;5(3):220-5. PMID 12553889.
Shahiwala A, Vyas TK, Amiji MM. Nanocarriers for systemic and mucosal vaccine delivery. Recent Pat Drug Deliv Formul. 2007;1(1):1-9. doi: 10.2174/187221107779814140, PMID 19075870.
Lee VH. Enzymatic barriers to peptide and protein absorption. Crit Rev Ther Drug Carrier Syst. 1988;5(2):69-97. PMID 3052875.
Allemann E. Polymeric nano- and microparticles for the oral delivery of peptides and peptidomimetics. Adv Drug Deliv Rev. 1998;34(2-3):171-89. doi: 10.1016/S0169-409X(98)00039-8.
Yoshioka T, Sternberg B, Florence AT. Preparation and properties of vesicles (niosomes) of sorbitan monoesters (Span 20, 40, 60, and 80) and a sorbitan triester (Span 85). International Journal of Pharmaceutics. 1994;105(1):1-6. doi: 10.1016/0378-5173(94)90228-3.
Gugleva V, Michailova V, Mihaylova R, Momekov G, Zaharieva MM, Najdenski H, et al. Formulation and evaluation of hybrid niosomal in situ Gel for intravesical co-delivery of curcumin and gentamicin sulfate. Pharmaceutics. 2022;14(4):747. doi: 10.3390/pharmaceutics14040747, PMID 35456581.
Li D, Martini N, Wu Z, Chen S, Falconer JR, Locke M, et al. Niosomal nanocarriers for enhanced dermal delivery of epigallocatechin gallate for protection against oxidative stress of the skin. Pharmaceutics. 2022;14(4):726. doi: 10.3390/pharmaceutics14040726, PMID 35456560.
Parthasarathi G, Udupa N, Umadevi P, Pillai GK. Niosome encapsulated of vincristine sulfate: improved anticancer activity with reduced toxicity in mice. J Drug Target. 1994;2(2):173-82. doi: 10.3109/10611869409015907, PMID 8069596.
Published
How to Cite
Issue
Section
Copyright (c) 2023 Gowtham Menon, Ravindra C Sutar, Sachin CP, Shendge R S, Girish A Kashid
This work is licensed under a Creative Commons Attribution-NonCommercial 4.0 International License.
