Design, Optimization and Characterization of Self-Nanoemulsifying Drug Delivery Systems of Bilastine
DOI:
https://doi.org/10.31351/vol32issSuppl.pp164-176Keywords:
Bilastine, SNEDDSAbstract
Self-nanoemulsifying drug delivery systems are innovative methods that have the potential to resolve a variety of drug formulation issues, including solubility, stability and bioavailability. Bilastine is a potent and highly selective H1-antihistamine. The aim of this study is to develop bilastine as an oral self-nanoemulsion to enhance its permeability from prepared formulas and possibility of lymphatic transport. Based on the solubility investigations of bilastine in some oils, surfactants and cosurfactants, fifteen formulae of liquid SNEDDS were created utilizing oleic acid, tween 60 and transcutol as oil, surfactant and co-surfactant respectively. Pseudoternary phase diagrams were used to evaluate the component phase behavior and the area of the nanoemulsion. The prepared formulas were evaluated for particle size, polydispersity index, zetapotential, self-emulsification time, drug content, and robustness to dilution. When compared to the pure drug powder, the produced SMEDDS formulations showed enhanced drug release. This study's findings showed that a formula 8 with a 20% oleic acid, 40% tween 60, and 40% transcutol composition exhibited lower particle size and higher zetapotential with acceptable drug content compared to other formulas and better in-vitro drug release characteristics than pure bilastine powder. All of these criteria favor the development of self-nano emulsifying drug delivery systems as a potential approach to enhance the bioavailability of drugs like bilastine that are poorly soluble.
Keywords: Bilastine, SNEDDS
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Ochoa D, Román M, Belmonte C, Martín-Vilchez S, Mejía-Abril G, Abad-Santos F, Hernández G, Arranz P, Elgezabal L, Fernández N. Pharmacokinetics and Safety of a Bilastine Once-Daily, Preservative-Free, Ophthalmic Formulation. Advances in Therapy. 2021 Jul;38(7):4070-81.
Wolthers OD. Bilastine: a new nonsedating oral H1 antihistamine for treatment of allergic rhinoconjunctivitis and urticaria. BioMed Research International. 2013 Jan 1;2013.
Narkhede SB, Dolly S, Talele AN, Prajapati AP. Formulation development and evaluation of sublingual drug delivery system of Bilastine for allergic rhinoconjuctivitis. IAJPS 2021 Apr;8(4):166-181.
Vozmediano V, Sologuren A, Lukas JC, Leal N, Rodriguez M. Model informed pediatric development applied to bilastine: ontogenic PK model development, dose selection for first time in children and PK study design. Pharmaceutical Research. 2017 Dec;34:2720-34.
Sádaba B, Gómez-Guiu A, Azanza JR, Ortega I, Valiente R. Oral availability of bilastine. Clinical drug investigation. 2013 May;33:375-81.
Al-Tamimi DJ, Hussein AA. Formulation and characterization of self-microemulsifying drug delivery system of tacrolimus. Iraqi Journal of Pharmaceutical Sciences (P-ISSN 1683-3597 E-ISSN 2521-3512). 2021 Jun 15;30(1):91-100.
Nair AB, Singh B, Shah J, Jacob S, Aldhubiab B, Sreeharsha N, Morsy MA, Venugopala KN, Attimarad M, Shinu P. Formulation and evaluation of self-nanoemulsifying drug delivery system derived tablet containing sertraline. Pharmaceutics. 2022 Jan 31;14(2):336.
Ghareeb MM, Neamah AJ. Formulation and characterization of nimodipine nanoemulsion as ampoule for oral route. International Journal of Pharmaceutical Sciences and Research. 2017 Feb 1;8(2):591.
Nasr AM, Gardouh AR, Ghonaim HM, Ghorab MM. Design, formulation and in-vitro characterization of Irbesartan solid self-nanoemulsifying drug delivery system (S-SNEDDS) prepared using spray drying technique. J Chem Pharm Res. 2016;8(2):159-83.
Mahmoud H, Al-Suwayeh S, Elkadi S. Design and optimization of self-nanoemulsifying drug delivery systems of simvastatin aiming dissolution enhancement. Afr J Pharm Pharmacol. 2013;7(22):1482-500.
Al-Tamimi DJ, Hussein AA. Formulation and characterization of self-microemulsifying drug delivery system of tacrolimus. Iraqi Journal of Pharmaceutical Sciences (P-ISSN 1683-3597 E-ISSN 2521-3512). 2021 Jun 15;30(1):91-100.
Alothaid H, Aldughaim MS, Yusuf AO, Yezdani U, Alhazmi A, Habibullah MM, Khan MG. A comprehensive study of the basic formulation of supersaturated self-nanoemulsifying drug delivery systems (SNEDDS) of albendazolum. Drug Delivery. 2021 Jan 1;28(1):2119-26.
Chandan C, Maheshwari RK. Mixed solvency concept in reducing surfactant concentration of self†emulsifying drug delivery systems of candesartan cilexetil using D†optimal mixture design. Asian Journal of Pharmaceutics (AJP). 2013;7(2).
Sabri LA, Hussein AA. Comparison between Conventional and Supersaturable Self-nanoemulsion Loaded with Nebivolol: Preparation and In-vitro/Ex-vivo Evaluation. Iraqi Journal of Pharmaceutical Sciences (P-ISSN: 1683-3597, E-ISSN: 2521-3512). 2020 Jun 25;29(1):216-25.
Ali HH, Hussein AA. Oral nanoemulsions of candesartan cilexetil: formulation, characterization and in vitro drug release studies. AAPS Open. 2017; 3(1):4.
Fadhel AY, Rajab NA. Tizanidine Nano emulsion: Formulation and in-vitro Characterization. Journal of Pharmaceutical Negative Results. 2022 Sep 16;13(3):572-81.
Prajapat MD, Patel NJ, Bariya A, Patel SS, Butani SB. Formulation and evaluation of self-emulsifying drug delivery system for nimodipine, a BCS class II drug. Journal of Drug Delivery Science and Technology. 2017;39:59-68.
Salim FF, Rajab NA. Formulation and Characterization of Piroxicam as Self-Nano Emulsifying Drug Delivery System. Iraqi Journal of Pharmaceutical Sciences (P-ISSN 1683-3597 E-ISSN 2521-3512). 2020 Jun 25;29(1):174-83.
Dahash RA, Rajab NA. Formulation and Investigation of Lacidipine as a Nanoemulsions. Iraqi Journal of Pharmaceutical Sciences (P-ISSN 1683-3597 E-ISSN 2521-3512). 2020 Jun 21;29(1):41-54.
Teaima M, Hababeh S, Khanfar M, Alanazi F, Alshora D, El-Nabarawi M. Design and optimization of pioglitazone hydrochloride self-nanoemulsifying drug delivery system (SNEDDS) incorporated into an orally disintegrating tablet. Pharmaceutics. 2022 Feb 16;14(2):425.
Verma R, Kaushik A, Almeer R, Rahman MH, Abdel-Daim MM, Kaushik D. Improved pharmacodynamic potential of rosuvastatin by self-nanoemulsifying drug delivery system: An in vitro and in vivo evaluation. International Journal of Nanomedicine. 2021;16:905.
Bakhle SS, Avari JG. Development and characterization of solid self-emulsifying drug delivery system of cilinidipine. Chem Pharm Bull 2015; 63(6): 408-17.
Inugala S, Eedara BB, Sunkavalli S, Dhurke R, Kandadi P, Jukanti R, et al. Solid self-nanoemulsifying drug delivery system (SSNEDDS) of darunavir for improved dissolution and oral bioavailability: In vitro and in vivo evaluation. Eur J Pharm Sci. 2015; 74:1-10.
Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profile. Eur J Pharm Sci 2001May; 13(2): 123-33.
Shrestha B, Dunn L. The Declaration of Helsinki on Medical Research involving Human Subjects: A Review of Seventh Revision. J Nepal Health Res Counc. 2020 Jan 21;17(4):548-552. doi: 10.33314/jnhrc.v17i4.1042. PMID: 32001865.
Garber JC, Barbee RW, Bielitzki JT, Clayton LA, Donovan JC, Hendriksen CFM, et al. Guide for the care and use of laboratory animals. Natl Aca Press Wash DC 2011;8:220.
Nair AB, Shah J, Aljaeid BM, Al-Dhubiab BE, Jacob S. Gellan gum-based hydrogel for transdermal delivery of nebivolol: Optimization and evaluation. Polymers 2019 Oct 16; 11(10): 1699.
Huang Y-B, Tsai Y-H, Yang W-C, CHANG JS, WU P-C. Guidance for industry, dissolution testing of immediate release solid oral dosage forms Guidance for industry, dissolution testing of immediate release solid oral dosage forms, 1997. Biological & pharmaceutical bulletin 2004;27(10):1626–9.
https://patentimages.storage.googleapis.com/91/6c/91/aaf201c8ff92e2/US20100004285A1.pdf
Sohn Y, Lee SY, Lee GH, Na YJ, Kim SY, Seong I, et al. Development of self-microemulsifying bilayer tablets for pHindependent fast release of candesartan cilexetil. Die Pharmazie. 2012; 67(11): 917-24.
Algahtani MS, Ahmad MZ, Ahmad J. Investigation of Factors Influencing Formation of Nanoemulsion by Spontaneous Emulsification: Impact on Droplet Size, Polydispersity Index, and Stability. Bioengineering. 2022 Aug 12;9(8):384.
Algahtani MS, Ahmad MZ, Nourein IH, Albarqi HA, Alyami HS, Alyami MH, Alqahtani AA, Alasiri A, Algahtani TS, Mohammed AA, Ahmad J. Preparation and characterization of curcumin nanoemulgel utilizing ultrasonication technique for wound healing: In vitro, ex vivo, and in vivo evaluation. Gels. 2021 Nov 14;7(4):213.
Khatri P, Shao J. Mechanism and structural factors of lipid and surfactant in the formation of self-emulsified nanoemulsion. J Pharm Sci. 2018; 107(8):2198-2207.
Ammar H, Ghorab MM, Mostafa D, Ghoneim AM. Selfnanoemulsifying drug delivery system for sertraline hydrochloride: Design, Preparation and characterization. Int J Pharm Pharm Sci. 2014; 6:589-95.
Amin MM, El Gazayerly ON, Abd El-Gawad NA, Abd El-Halim SM, El-Awdan SA. Effect of formulation variables on design, in vitro evaluation of valsartan SNEDDS and estimation of its antioxidant effect in adrenaline-induced acute myocardial infarction in rats. Pharm Dev Technol. 2016; 21(8):909-20.
Inugala S, Eedara BB, Sunkavalli S, Dhurke R, Kandadi P, Jukanti R, et al. Solid self-nanoemulsifying drug delivery system (SSNEDDS) of darunavir for improved dissolution and oral bioavailability: In vitro and in vivo evaluation. Eur J Pharm Sci. 2015; 74:1-10.
Parmar N, Singla N, Amin S, Kohli K. Study of cosurfactant effect on nanoemulsifying area and development of lercanidipine loaded (SNEDDS) self nanoemulsifying drug delivery system. Colloids Surf B, Biointerfaces. 2011; 86(2):327-38.
Saifullah S, Kanwal T, Ullah S, Kawish M, Habib SM, Ali I, Munir A, Imran M, Shah MR. Design and development of lipid modified chitosan containing muco-adhesive self-emulsifying drug delivery systems for cefixime oral delivery. Chemistry and Physics of Lipids. 2021 Mar 1;235:105052.
Mekhilef SF, Hussein AA. Novel combination for selfnanoemulsifying drug delivery system of candesartan cilexetil. Iraqi J Pharm Sci. 2018; 27(2):123-34.
Fitria A, Hanifah S, Chabib L, Uno AM, Munawwarah H, Atsil N, Pohara HA, Weuanggi DA, Syukri Y. Design and characterization of propolis extract loaded self-nano emulsifying drug delivery system as immunostimulant. Saudi Pharmaceutical Journal. 2021 Jun 1;29(6):625-34.
Villalobos-Hernández JR, Müller-Goymann CC. Novel nanoparticulate carrier system based on carnauba wax and decyl oleate for the dispersion of inorganic sunscreens in aqueous media. European journal of pharmaceutics and biopharmaceutics. 2005 May 1;60(1):113-22.
Chaudhary S, Aqil M, Sultana Y, Kalam MA. Self-nanoemulsifying drug delivery system of nabumetone improved its oral bioavailability and anti-inflammatory effects in rat model. Journal of Drug Delivery Science and Technology. 2019 Jun 1;51:736-45.
Balakumar K, Raghavan CV, selvan NT, prasad RH, Abdu S. Self nanoemulsifying drug delivery system (SNEDDS) of rosuvastatin calcium: design, formulation, bioavailability and pharmacokinetic evaluation. Colloids Surf B, Biointerfaces. 2013; 112:337-43.
Singh D, Tiwary A, Bedi N. Canagliflozin loaded SMEDDS: formulation optimization for improved solubility, permeability and pharmacokinetic performance. J Pharm Invest. 2018; 49:67-85.
Reddy MR, Gubbiyappa KS. Formulation development, optimization and characterization of Pemigatinib-loaded supersaturable self-nanoemulsifying drug delivery systems. Future Journal of Pharmaceutical Sciences. 2022 Nov 12;8(1):45.
The United States Pharmacopoeia (USP) 30 N. NF 25. The United States Pharmacopeial Convention Inc. USA: Rockville; 2006. P.1191- 3, 2110.
Wu W, Wang Y, Que L. Enhanced bioavailability of silymarin by selfmicroemulsifying drug delivery system. European Journal of Pharmaceutics and Biopharmaceutics 2006;63(3):288–94.
Bakhle SS, Avari JG. Development and characterization of solid self-emulsifying drug delivery system of cilinidipine. Chem Pharm Bull 2015; 63(6): 408-17.
Park EJ, Choi SA, Min KA, Jee JP, Jin SG, Cho KH. Development of Alectinib-Suspended SNEDDS for Enhanced Solubility and Dissolution. Pharmaceutics. 2022 Aug 14;14(8):1694.
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