NOVEL UMBELLIFERONE PHYTOSOMES: DEVELOPMENT AND OPTIMIZATION USING EXPERIMENTAL DESIGN APPROACH AND EVALUATION OF PHOTO-PROTECTIVE AND ANTIOXIDANT ACTIVITY
DOI:
https://doi.org/10.22159/ijpps.2017v9i1.14635Keywords:
Umbelliferone phytosome, Solvent evaporation, Box-Behnken design, Partition coefficient, Solubility, Antioxidant activity, Photo-protective activityAbstract
Objective: The objective of this study was to develop a novel formulation (Phytosome) of umbelliferone with phospholipid for improved permeability, solubility and hence better pharmacological action.
Methods: The phytosomal complex was prepared by using solvent evaporation method and optimised by applying the Box-Behnken design on the basis of complexation rate and partition coefficient. The formation of phytosomes was confirmed by FTIR, DSC, SEM, XRD, HPTLC and NMR by comparing the results of the complex with the drug. The photoprotective potential of complex against UV-exposure was evaluated in rats and compared with the drug by incorporating it in a gel and estimating the antioxidant enzymes in skin namely reduced glutathione, superoxide dismutase, lipid peroxidation and catalase.
Results: The crystalline drug was completely converted to amorphous complex. The complex showed a good practical yield, drug content and particle size was in the range. The solubility of the complex was determined by partition coefficient method and was found to be better than the drug. The ex vivo and in-vitro permeation of the complex showed improved permeation for complex than the drug. The in vitro antioxidant activity of complex was evaluated by DPPH and ferrozine antioxidant assay and was better than the drug. The photoprotective action of the complex was found to be better than drug on the basis of the content of antioxidant enzymes estimated in the skin.
Conclusion: The phytosomal complex was found to show better solubility in the water phase and oil phase, better permeation, better antioxidant activity and a better photo-protective activity when compared to umbelliferone.Downloads
References
Kalita B, Das MK, Sharma AK. Novel phytosome formulations in making herbal extracts more effective. Res J Pharm Technol 2013;6:1295-301.
More MS, Shende M, Kolhe DB, Jaiswal NM. Herbosomes: herbo-phospholipid complex an approach for absorption enhancement. Int J Biol Pharm Res 2012;3:946-55.
Choubey A. Phytosome–a novel approach for herbal drug delivery. Int J Pharm Sci Res 2011;2:807-15.
Chein YW. Novel Drug Delivery Systems. Second ed. 1; 2011. p. 816.
Sarangi MK, Padhi S. Solid lipid nanoparticles-a review. J Crit Rev 2016;3:5-12.
Patel J, Patel R, Khambolja K, Patel N. An overview of phytosomes as an advanced herbal drug delivery system. Asian J Pharmacol 2009;4:363-71.
Tripathy S, Patel DK, Baro L, Nair SK. A review on phytosomes, their characterization, advancement and potential for transdermal application. J Drug Delivery Ther 2013;3:147-52.
Gandhi A, Dutta A, Pal A, Bakshi P. Recent trends of phytosomes for delivering herbal extract with improved bioavailability. J Pharmacogn Phytochem 2012;1:1-14.
Jain N, Gupta BP, Thakur N, Jain R, Banweer J, Jain DK, et al. Phytosome: a novel drug delivery system for herbal medicine. Int J Pharm Sci Res 2010;2:224-8.
Malik A, Kushnoor A, Saini V, Singhal S, Kumar S, Yadav YC. Analytical method development of nutraceutical: umbelliferone. Int J Pharm Sci 2012;3:67-73.
Kokate CK, Purohit AP, Gokhale SB. Pharmacognosy. 31st ed. Nirali Prakashan; 2005. p. 596.
Oviya VJ, Vishnupriya V, Gayathri R. Comparative analysis of antioxidant and free radicals scavenging activity of lemongrass oil and lavender oil. Asian J Pharm Clin Res 2016;9:136-9.
Furniss BS, Hannaford AJ, Smith PWG, Tatchell AR. Vogel’s Textbook. 5th ed. Practical Organic Chemistry; 2008. p. 236-40.
Rawat MSM, Semalty A, Semalty M, Singh D. Preparation and characterization of phospholipid complexes of naringenin for effective drug delivery. Springer Sci 2010;67:253-60.
Singh S, Mishra A, Verma A, Ghosh AK, Mishra AK. A simple ultraviolet spectrophotometric method for the determination of etoricoxib in dosage formulations. J Adv Pharm Technol Res 2012;5:237-40.
Saharan VA, Agarwal A, Kharb V. Process optimisation, characterization and evaluation of resveratrol-phospholipid complexes using box-behnken statistical design. Int Curr Pharm J 2014;3:301-8.
Tan Q, Liu S, Chen X, Wu M, Wang H, Yin H, et al. Design and evaluation of a novel evodiamine-phospholipid complex for improved oral bioavailability. AAPS PharmSciTech 2012; 13:534-47.
Sikarwar MS, Sharma S, Jain AK, Parial SD. Preparation, characterization and evaluation of marsupsin-phospholipid complex. AAPS PharmSciTech 2008;9:129–37.
Nickilisch SCT, Waite JH. Optimised DPPH assay in a detergent-based buffer system for measuring antioxidant activity of proteins. Methods X, Elsevier 2014;1:233-8.
Santhy KS, Archana D, Dixitha M. Antioxidant and anticlastogenic potential of Piper longum L. Int J Appl Pharm 2015;7:11-4.
Pandey KD, Kumar A, Singh M, Singh PP, Singh SK, Raj P. Antioxidant efficacy and curcumin content of turmeric (Curcuma longa L.) flower. Int J Curr Pharm Res 2016;8:112-4.
Semalty A, Semalty M, Singh D, Rawat MSM. The phyto-phospholipid complex of catechin in value added herbal drug delivery. J Inclusion Phenom Macrocyclic Chem 2012;73:377-86.
Dringen R, Riemer J, Hoepken HH, Czerwinska H, Robinson SR. Colorimetric ferrozine-based assay for the quantitation of iron in cultured cells. Anal Biochem Elsevier 2004; 331:370-5.
Dhalwal K, Shinde VM, Mahadik KR, Namdeo AG. A rapid densitometric method for simultaneous analysis of umbelliferone, psoralen, and eugenol in herbal raw materials using HPTLC. J Sep Sci 2007;30:2053-8.
Husain A, Aamir M, Mujeeb M, Siddique NA. Simultaneous quantification of umbelliferone and quercetin in polyherbal formulations of Aegle marmelos by HPTLC. Am J PharmTech Res 2012;2:2249-3387.
Yue PF, Yuan H, Li X, Yang M, Zhu W. Process optimisation, characterization and evaluation in vivo of the oxymatrine-phospholipid complex. Int J Pharm 2010;387:139-46.
Mukherjee PK, Bhattacharyya S, Majhi S, Saha BP. Chlorogenic acid-phospholipid complex improve protection against UVA-induced oxidative stress. J Photochem Photobiol B 2014;130:293-8.
Ahmed AB, Ahmed R, Sengupta R. Formulation and in vitro/ex-vivo characterizations of microemulsion-based hydrogel formulation of aceclofenac for topical application. Asian J Pharm Clin Res 2016;9:87-91.
Rawat MSM, Singh D, Semalty A, Semalty M. Emodin-phospholipid complex-A potential of herbal drug in the novel drug delivery system. J Therm Anal Calorim Springer Sci 2012;108:289-98.
Pretsch E, Buhlmann P, Badertscher M. Structure determination of organic compounds. Tables of Spectral Data, Springer Sci 2009;4:93-108.
Das S, Haldar PK, Pramanik G. Formulation and evaluation of herbal gel containing Clerodendron infortunatum leaves extract. Int J PharmTech Res 2011;3:140-3.
Kumar TG, Kaur LP. Formulation and evaluation of topical gel of aceclofenac. J Drug Delivery Ther 2013;3:51-3.
Sharma S, Kaur IP. Development and evaluation of sesamol as an antiaging agent. Int J Dermatol 2006;45:200–8.
Rahman H, Muralidharan P, Anand M. Inhibition of AChE and antioxidant activities are a probable mechanism of Nardostacys jatamansi DC in sleep deprived Alzheimer's mice model. Int J PharmTech Res 2011;3:1807-16.
Beutler E, Duron O, Kelly BM. An improved method for the determination of blood glutathione. J Lab Clin Med 1963;61:882-8.
Misra HP, Fridovich I. The oxidation of phenylhydrazine: superoxide and mechanism. Biochemistry 1976;15:681-7.
Aebi H. Methods of enzymatic analysis. ed. New York, Academic Press; 1974;2:674.
Ohkawa H, Ohisi N, Yagi K. Assay for lipid peroxides in animal tissues by thiobarbituric acid reaction. Anal Biochem 1979;95:351-8.
Li Y, Wu H, Jia M, Cui F, Lin J, Yang X, et al. Therapeutic effect of folate-targeted and PEGylated phytosomes loaded with a mitomycin c-soybean phosphatidylcholine complex. Mol Pharm 2014;11:3017-26.
Mukherjee P, Maiti K, Mukherjee K, Gantait A, Saha B. Curcumin-phospholipid complex: preparation, therapeutic evaluation and pharmacokinetic study in rats. Int J Pharm 2007;330:155-63.
Skoog D, West D. Principles of instrumental analysis saunders golden sunburst series. 2nd ed; 1992. p. 221-54.
Pavia D, Lampman G, Kriz G, Vyvyan J. Introduction to spectroscopy. 4th ed; 1996. p. 142-60.