DESIGN AND DEVELOPMENT OF PHYTOSOMAL SOFT NANOPARTICLES FOR LIVER TARGETING
Keywords:Ferulic acid, Conjugation, Complex formation, Solvent evaporation method, Solvent evaporation technique, Nanoparticle, Drug targeted systems, Bioavailability
Objective: The objective of the study was to design and formulate ferulic acid (FA) phytosomes converted in to functionalised soft nanoparticles by using the solvent evaporation method to increase resistance time, improve the bioavailability and half-life of ferulic acid.
Methods: FA is a BCS-II drug, which has low solubility and high permeability. The functionalised soft nanoparticles was prepared by the solvent evaporation method followed by the particle size and zeta potential, Fourier Transform Infra-Red (FTIR), Powder x-Ray Diffraction (PXRD), Scanning Electron Microscope (SEM). It indicates good result for the complexation rate. PXRD showed good powder diffraction results with having good flow property. Particle size and zeta potential had a good result of-12.05±120 improved by the cationic polymer. The complex was evaluated by the study of drug loading, entrapment efficiency, histopathological study and mucoadhesive property for the final formulation of the microspheres system. Also, the formulation were evaluated for the In vitro drug dissolution study for rate of the extent of drug release. Ex-vivo drug diffusion study by using goat nasal mucosa using pH 6.6 for evaluating rate of the extent of drug diffusion through nasal mucosa.
Results: The results of the characterization studies indicated the designing of functionalised phytosomal soft nanoparticles (FPSN). The FPSN particle size and zeta potential had a good result of-12.05±120. The FTIR spectra of the complex showed a characteristic peak at 3652.8 cm-1(OH-stretching) which indicate that the shifting and interaction between the FA and soya phospholipid complex (SPC 3). The P-XRD, SEM, In vitro dissolution showed good powder diffraction results with having good flow property. The complex is evaluated by the study of drug loading. Also formulation were evaluated for the In vitro drug dissolution study for rate of the extent of drug release. The result of the above studies was Drug loading increased at 44.42 %. The Ex-vivo permeation study ferulic acid-phytosomal soft nanoparticle (FALC-PSN) showed characteristic in the drug diffusion at 80.04 %, which indicate that the drug had increases its aqueous solubility and also change with the structural morphology.
Conclusion: It can be concluded that the ferulic acid phytosomal soft nanoparticles (FAPSN) enhance the solubility of the FA and increased the bioavailability and retention time to target liver cancer.
Alpar HO, Somavarapu S, Atuah KN, Bramwell VW. Biodegradable mucoadhesive particulates for nasal and pulmonary antigen and DNA delivery. Adv Drug Deliv Rev. 2005;57(3):411-30. doi: 10.1016/j.addr.2004.09.004, PMID 15560949.
Tas C, Ozkan CKose, Savaser A, Ozkan Y, Tasdemir U, Hikmetal Tunay. Nasal absorption of metoclopramide from different Carbopol 981 based formulations: in vitro, ex vivo and in vivo evaluation. doi: 10.1016/j.ejpb.2006.05.017.
Chandna A, Batra D, Kakar S, Singh R. A review on target drug delivery: magnetic microspheres. Journal of Acute Disease. 2013;2(3):189-95. doi: 10.1016/S2221-6189(13)60125-0.
Hemant K, Abhay R, Praveen S, Swati U, Hemanth KS. Cancer nanotechnology: nanoparticulate drug delivery for the treatment of cancer. Int J Pharm Pharm Sci 2020;7(3):40-6.
Chandan A, Batra D, Kakar R, Singh A. Review on target drug delivery: magnetic microspheres. Journal of Acute Disease. 2013;2(3):189–95. doi: 10.1016/S2221-6189;13:60125-0.
Cota Arriola O, Plascencia Jatomea M, Lizardi Mendoza J, Robles Sanchez RM, Ezquerra Brauer JM, Ruiz Garcia J. Preparation of chitosan matrices with ferulic acid: physicochemical characterization and relationship on the growth of Aspergillus parasiticus. CyTA Journal of Food 2016:1-10. doi: 10.1080/19476337.2016.1213317.
Raju SK, Karunakaran A, Kumar S, Sekar P, Murugesan M, Karthikeyan M. Biogenic synthesis of copper nanoparticles and their biological applications: an overview. Int J Pharm Pharm Sci. 2022;14(3):8-26. doi: 10.22159/ijpps.2022v14i3.43842.
Khan YY, Suvarna V. Liposomes containing phytochemicals for cancer treatment-an update. Int J Curr Pharm Sci 2017;9(1). doi: 10.22159/ijcpr.2017v9i1.16629.
Telange DR, Patil AT, Pethe AM, Fegade H, Anand S, Dave VS. Formulation and characterization of an apigenin-phospholipid phytosome (APLC) for improved solubility, in vivo bioavailability, and antioxidant potential. Eur J Pharm Sci. 2017;108:36-49. doi: 10.1016/j.ejps.2016.12.009. PMID 27939619.
Sivapriya V, Ponnarmadha S, Azeezand NA, Sudarshanadeepa V. Novel nanocarriers for ethnopharmacological formulations. Int J App Pharm. 2018;10(4):26-30. doi: 10.22159/ijap.2018v10i4.26081.
Gupta S, Samanta MK, Raichur AM. Dual-drug delivery system based on in situ gel-forming nanosuspension of forskolin to enhance antiglaucoma efficacy. AAPS PharmSciTech. 2010;11(1):322-35. doi: 10.1208/s12249-010-9388-x, PMID 20182824.
Hascicek C, Gonul N, Erk N. Mucoadhesive microspheres containing gentamicin sulfate for nasal administration: preparation and in vitro characterization. Farmaco. 2003 Jan;58(1):11-6. doi: 10.1016/S0014-827X(02)00004-6.
He P, Davis SS, Illum L. Sustained release chitosan microspheres prepared by novel spray drying methods. J Microencapsul. 1999 May-Jun;16(3):343-55. doi: 10.1080/026520499289068, PMID 10340219.
Hermens WAJJ, Merkus FWHM. The influence of drugs on nasal ciliary movement. Pharm Res. 1987;4(6):445-9. doi: 10.1023/a:1016463118748. PMID 3334167.
Illum L. Is nose-to-brain transport of drugs in man a reality? J Pharm Pharmacol. 2004;56:3-17. doi: 10.1211/0022357022539, PMID 14979996.
Illum L. Nasal drug delivery-possibilities, problems and solutions. J Control Release. 2003 Feb 21;87(1-3):187-98. doi: 10.1016/s0168-3659(02)00363-2, PMID 12618035.
Kakar S, Batra D, Singh R, Nautiyal U. Magnetic microspheres as magical novel drug delivery system: a review. J Acute Dis. 2013;2(1):1-12. doi: 10.1016/S2221-6189(13)60087-6.
Karthivashan G, Masarudin MJ, Kura AU, Abas F, Fakurazi S. Optimization, formulation, and characterization of multiflavonoids-loaded flavanosome by bulk or sequential technique. Int J Nanomedicine. 2016 Jul 27;11:3417-34. doi: 10.2147/IJN.S112045. PMID 27555765.
Koyani V, Dedaka P, Matholiya P. Microspheres for intransal deliver system: as review. J of Informa Health Care. 2014;2(1).
Meredith ME, Salameh TS, Banks WA. Intranasal delivery of proteins and peptides in the treatment of neurodegenerative diseases. AAPS J. 2015;17(4):780-7. doi: 10.1208/s12248-015-9719-7. PMID 25801717.
Mistry A, Glud SZ, Kjems J, Randel J, Howard KA, Stolnik S. Effect of physicochemical properties on intranasal nanoparticle transit into murine olfactory epithelium. J Drug Target. 2009;17(7):543-52. doi: 10.1080/10611860903055470, PMID 19530905.
Miyake MM, Bleier BS. The blood-brain barrier and nasal drug delivery to the central nervous system. Am J Rhinol Allergy. 2015;29(2):124-7. doi: 10.2500/ajra.2015.29.4149, PMID 25785753.
Pristis E, Dhommat R, Jain A, Swami Challa VG, Shaheen M, Khan W. Intranasal delivery of nanoparticle encapsulated tarenflurbil: A potential brain targeting strategy for Alzheimer’s diseases. Eur J Pharm Sci. 2016 May:1-36. doi: 10.1016/j.ejps.2016.05.012.
Murata Y, Miyamoto E, Kawashima S. Additive effect of chondroitin sulfate and chitosan on drug release from calcium-induced alginate gel beads. J Control Release. 1996;38(2-3):101-8. doi: 10.1016/0168-3659(95)00098-4.
Patel MR, Patel RB, Bhatt KK, Patel BG, Gaikwad RV. Paliperidone microemulsion for nose-to-brain targeted drug delivery system: pharmacodynamic and pharmacokinetic evaluation. Drug Deliv. 2016;23(1):346-54. doi: 10.3109/10717544.2014.914602, PMID 24865295.
Patil SB, Sawant KK. Chitosan microspheres as a delivery system for nasal insufflations. Colloids Surf B Biointerfaces. 2011;84(2):384-9. doi: 10.1016/j.colsurfb.2011.01.030, PMID 21320767.
Jeevana Jyothi B, Mary Ragalatha P. Development and in vitro evaluation of phytosomes of naringin. Asian J Pharm Clin Res 2019;12(9):252-6. doi: 10.22159/ajpcr.2019.v12i9.34798.
Robinson N, Garabowski P, Rehman I. Alzheimer disease pathogenesis: is there a role of folate. Mech Ageing Dev. 2017 Oct 5:86-94. doi: 10.1016/j.mad.2017.10.001.
Shah S, Qaqish R, Patel V, Amiji M. Evaluation of the factors influencing stomach-specific delivery of antibacterial agents for Helicobacter pylori infection. J Pharm Pharmacol. 1999 Jun;51(6):667-72. doi: 10.1211/0022357991772952, PMID 10454042.
Shingaki T, Inoue D, Furubayashi T, Sakane T, Katsumi H, Yamamoto A. Transnasal delivery of methotrexate to brain tumors in rats: a new strategy for brain tumor chemotherapy. Mol Pharm. 2010;7(5):1561-8. doi: 10.1021/mp900275s. PMID 20695463.
Trombino S, Serini S, Di Nicuolo F, Celleno L, Ando S, Picci N. Antioxidant effect of ferulic acid in isolated membrane and intact cells: synergistic interaction with α-Tocopherol, β-carotene and ascorbic acid. J Agric Food Chem. 2004 Mar 20;52(8):2411-20. doi: 10.1021/jf0303924, PMID 15080655.
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