Modeling of ticagrelor bioadhesive solid dispersion based on coaxial electrostatic spray to enhance oral bioavailability and improve drug release
Main Article Content
Keywords
Uniaxial electrostatic spray Ticagrelor, coaxial electrostatic spray, bioadhesion, solid dispersion
Abstract
In order to address ticagrelor's (TIC) low solubility and poor bioavailability, the current study created a structured bioadhesive core-shell drug delivery system. The uniaxial electrostatic spray technique was used to create ticagreior solid dispersion (T-SD). The coaxial electrostatic spray method was also used to create ticagrelor bio adhesive solid dispersion (T-BSD). Using a biological adhesion test, the adhesion of T-BSD to each segment of the intestinal tract was identified. The plasma concentration-time curve and associated pharmacokinetic parameters were studied using the compartment model. The outcomes of bioadhesion tests revealed that T-BSD had a favorable adhesion effect in every intestinal segment. T-maximum BSD's plasma concentration (Cmax) increased from the free drug's (365ng/mL) level to 575.08ng/mL. The t1/2, MRT, and Tmax of T-BSD (12 h, 9.4h, and 4h, respectively) were all longer than those of the free drug (11.2h, 8.6h, and 1h). T-relative BSD's bioavailability increased even more in comparison to the free drug, reaching 430%. Collectively, the results showed that the coaxial-electrospray method might be a promising means of enhancing TIC's bioavailability.
References
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Alam, Abdul Ahad, Abdulmohsen A. Al-Saleh, Abdullah M and Al-Mohizea (2017). Pharmacodynamic study of eprosartan mesylate-loaded transfersomes Carbopol® gel under Dermaroller® on rats with methyl prednisolone acetate-induced hypertension. Biomed Pharmacother. 89(36):177-184.
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Chen R, Zhai R, Wang C, Liang S, Wang J, Liu Z and Li WL (2022). Compound capecitabine colon-targeted microparticle prepared by coaxial electrospray for treatment of colon tumors. Molecules. 27(17): 5690.
Dormer NH, Gupta V, Scurto AM, Scurto AM, Berkland CJ and Detamore MS (2013). Effect of different sintering methods on bioactivity and release of proteins from PLGA microspheres. Mat. Sci. Eng. C., 33(7): 4343-4351.
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GU Chunmei, GAO Zhenyu and LU Jinmiao (2014). Discussion on the substitution of ticagrelor for clopidogrel. Shanghai Medical & Pharmaceutical Journal, 35(1): 20-21.
Hongfei Liu, Kunyu Du, Dongli Li, Yi Du, Jumei Xi, Yan Shen, Tao Jiang and Thomas J Webster (2018). A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology. Int. J. Nanomedicine. 13(16): 8379-8393.
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Ioanna Xanthopoulou, Ilianna Bei, Theodora Bampouri, Nikolaos Barampoutis, Athanasios Moulias, Periklis Davlouros and Dimitrios Alexopoulos (2018). Absence of differential effect of ticagrelor versus prasugrel maintenance dose on endothelial function in patients with stable coronary artery disease. Hellenic. J. Cardiol., 59(6): 338-343.
Joon Ho Ahn, Youngkeun Ahn, Myung Ho Jeong, Ju Han Kim, Young Joon Hong and Sun Sim (2020). Ticagrelor versus clopidogrel in acute myocardial infarction patients with multivessel disease. J. Cardiol., 75(5): 478-484.
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Leonardo C, Clavijo, Ashwat Dhillon, Ray V, Jorge Caro and Han Tun (2018). Switch to ticagrelor in critical limb ischemia antiplatelet study (STT-CLIPS). Cardiovasc. Revasc. Med. 19(3): 319-323.
Nath SD, Son S, Sadiasa A, Min YK and Lee BT (2013). Preparation and characterization of PLGA microspheres by the electrospraying method for delivering simvastatin for bone regeneration. Int. J. Pharmaceut., 443(1): 87-94.
Parhizkar LM and Reardon PJT (2017). Performance of novel high throughput multi electrospray systems for forming of polymeric micro/nanoparticles. MATER DESIGN. 126(1): 73-84.
Philippe Gabriel S, Stefan J and Harrington RA (2010). Ticagrelor versus clopidogrel in patients with STelevation acute coronary syndromes intended for reperfusion with primary percutaneous coronary intervention: A platelet inhibition and patient outcomes (PLATO) trial subgroup analysis. Circulation. 122(21): 2131-2141.
Sung-Jin Kim, Hong-Ki Lee, Young-Guk Na, Ki-Hyun Bang, Hye-Jin Lee and Miao Wang (2019). A novel composition of ticagrelor by solid dispersion technique for increasing solubility and intestinal permeability. Int. J. Pharm., 555(42): 11-18.
Sharvil Patil, Abhijeet Mahadik, Pradeep Nalawade and Pratyush More (2017). Crystal engineering of lactose using electrospray technology: Carrier for pulmonary drug delivery. Drug Dev. Ind. Pharm., 43(12): 2085- 2091.
Sachin Rathod, Rahul Tripathi and Gunjan Verma (2018). Bioadhesive polymeric film-based integrative platform for the unidirectional carbamazepine release from a volatile microemulsion. Colloid. Surface B. 170(26): 683-691.
Sultanova Z, Kaleli G, Kabay G, Mutlu M and Kabay ZG (2016). Controlled release of a hydrophilic drug from coaxially electrosprayed polycaprolactone nanofibers. Int. J. Pharm. 505(1-2): 133-138.
Takurou N. Murakami and Michael Gratzel (2007). Counter electrodes for DSC: Application of functional materials as catalysts. Inorganica. Chim. Acta., 361(3): 572-580.
Vinicius R, Acquaro Junior, Germán Augusto GomezRíos, Marcos Tascon and Queiroz Costa (2019). Analysis of endocannabinoids in plasma samples by biocompatible solid-phase microextraction devices coupled to mass spectrometry. Anal. Chim. Acta., 1091(73): 135-145.
Weihong Yin, Xiaojie Ju, Rui Xie, Wei Wang, Zhuang Liu and Liangyin Chu (2021). Dual drug-loaded coreshell microspheres for programmed sequential release. Chem. Eng. Prog., 40(2): 998-1007.
Wang Yan, MU Cong and Liu Jinfeng (2017). Effects of particle size of ticagrelor crude drug on in vivo dissolution behavior of ticagrelor tablet. China pharmacy. 28(1): 119-121.
Yadav M, Sarolia J, Vyas B, Lalan M, Mangrulkar S and Shah P (2021). Amalgamation of solid dispersion and melt adsorption technique: Improved In Vitro and In Vivo performance of ticagrelor tablets. AAPS Pharm. Sci. Tech., 22(8): 257.
Young-Guk Na, Jin-Ju Byeon, MiaoWang, Min-Ki Kim and Ki-Hyun Bang (2019). Statistical approach for solidifying ticagrelor loaded self-microemulsifying drug delivery system with enhanced dissolution and oral bioavailability. Mat. Sci. Eng. C., 104(27): 109980
Zhou L (2015). Construction of electrospinning sustainedrelease system with water-soluble drugs and Study on drug release. Su Zhou: Suzhou University.
Alam, Abdul Ahad, Abdulmohsen A. Al-Saleh, Abdullah M and Al-Mohizea (2017). Pharmacodynamic study of eprosartan mesylate-loaded transfersomes Carbopol® gel under Dermaroller® on rats with methyl prednisolone acetate-induced hypertension. Biomed Pharmacother. 89(36):177-184.
Adel Penhasi and Albert Reuveni (2019). Preparation and evaluation of a bio-erodible bio-adhesive drug delivery system designed for intraoral extended release of flurbiprofen: In vitro and in vivo assessments. J. Pharm. Innov., 14(1): 15-27.
Annelies Smeets, Ida Lo Re, Christian Clasen, Guy and Van den Mooter (2020). Fixed dose combinations for cardiovascular treatment via coaxial electrospraying: Coated amorphous solid dispersion particles. Int. J. Pharm., 577(43): 118949.
Chen Gang (2015). Research progress on ticagrelor in treatment of acute coronary syndrome china & foreign medical treatment. China & Foreign Medical Treatment. 24(35): 196-198.
Caren Gobetti, Rusia Lazzaretti Pereira, Andreas Sebastian Loureiro Mendez and Garcia CV (2014). Determination of the new antiplatelet agent ticagrelor in tablets by stability-indicating hplc method. Curr. Pharm. Anal., 10(4): 279-283.
Chen R, Zhai R, Wang C, Liang S, Wang J, Liu Z and Li WL (2022). Compound capecitabine colon-targeted microparticle prepared by coaxial electrospray for treatment of colon tumors. Molecules. 27(17): 5690.
Dormer NH, Gupta V, Scurto AM, Scurto AM, Berkland CJ and Detamore MS (2013). Effect of different sintering methods on bioactivity and release of proteins from PLGA microspheres. Mat. Sci. Eng. C., 33(7): 4343-4351.
Fatmanur Tugcu-Demiroz, Isabel Gonzalez-Alvarez, Marta Gonzalez-Alvarez and Marival Bermejo (2014). Validation of phenol red versus gravimetric method for water reabsorption correction and study of gender differences in Doluisio’s absorption technique. Eur. J. Pharm. Sci., 62(22): 105-110.
GU Chunmei, GAO Zhenyu and LU Jinmiao (2014). Discussion on the substitution of ticagrelor for clopidogrel. Shanghai Medical & Pharmaceutical Journal, 35(1): 20-21.
Hongfei Liu, Kunyu Du, Dongli Li, Yi Du, Jumei Xi, Yan Shen, Tao Jiang and Thomas J Webster (2018). A high bioavailability and sustained-release nano-delivery system for nintedanib based on electrospray technology. Int. J. Nanomedicine. 13(16): 8379-8393.
He T and Jokerst JV (2020). Structured micro/nano materials synthesized via electrospray: A review. Biomater. Sci., 8(20): 5555-5573.
Ioanna Xanthopoulou, Ilianna Bei, Theodora Bampouri, Nikolaos Barampoutis, Athanasios Moulias, Periklis Davlouros and Dimitrios Alexopoulos (2018). Absence of differential effect of ticagrelor versus prasugrel maintenance dose on endothelial function in patients with stable coronary artery disease. Hellenic. J. Cardiol., 59(6): 338-343.
Joon Ho Ahn, Youngkeun Ahn, Myung Ho Jeong, Ju Han Kim, Young Joon Hong and Sun Sim (2020). Ticagrelor versus clopidogrel in acute myocardial infarction patients with multivessel disease. J. Cardiol., 75(5): 478-484.
Jinkun Huang, Li Liang and Jiao Zuo (2017). Ticagrelor solid dispersion and preparation method thereof. WO/2015/039513. Jiaming Chen, Yuecheng Cui, Xin Xu and Liqun Wang (2018). Direct and effective preparation of core-shell PCL/PEG nanoparticles based on shell insertion strategy by using coaxial electrospray. Colloids and surfaces a: Physicochemical and engineering aspects. Colloid Surface A. 547(26): 1-7.
Leonardo C, Clavijo, Ashwat Dhillon, Ray V, Jorge Caro and Han Tun (2018). Switch to ticagrelor in critical limb ischemia antiplatelet study (STT-CLIPS). Cardiovasc. Revasc. Med. 19(3): 319-323.
Nath SD, Son S, Sadiasa A, Min YK and Lee BT (2013). Preparation and characterization of PLGA microspheres by the electrospraying method for delivering simvastatin for bone regeneration. Int. J. Pharmaceut., 443(1): 87-94.
Parhizkar LM and Reardon PJT (2017). Performance of novel high throughput multi electrospray systems for forming of polymeric micro/nanoparticles. MATER DESIGN. 126(1): 73-84.
Philippe Gabriel S, Stefan J and Harrington RA (2010). Ticagrelor versus clopidogrel in patients with STelevation acute coronary syndromes intended for reperfusion with primary percutaneous coronary intervention: A platelet inhibition and patient outcomes (PLATO) trial subgroup analysis. Circulation. 122(21): 2131-2141.
Sung-Jin Kim, Hong-Ki Lee, Young-Guk Na, Ki-Hyun Bang, Hye-Jin Lee and Miao Wang (2019). A novel composition of ticagrelor by solid dispersion technique for increasing solubility and intestinal permeability. Int. J. Pharm., 555(42): 11-18.
Sharvil Patil, Abhijeet Mahadik, Pradeep Nalawade and Pratyush More (2017). Crystal engineering of lactose using electrospray technology: Carrier for pulmonary drug delivery. Drug Dev. Ind. Pharm., 43(12): 2085- 2091.
Sachin Rathod, Rahul Tripathi and Gunjan Verma (2018). Bioadhesive polymeric film-based integrative platform for the unidirectional carbamazepine release from a volatile microemulsion. Colloid. Surface B. 170(26): 683-691.
Sultanova Z, Kaleli G, Kabay G, Mutlu M and Kabay ZG (2016). Controlled release of a hydrophilic drug from coaxially electrosprayed polycaprolactone nanofibers. Int. J. Pharm. 505(1-2): 133-138.
Takurou N. Murakami and Michael Gratzel (2007). Counter electrodes for DSC: Application of functional materials as catalysts. Inorganica. Chim. Acta., 361(3): 572-580.
Vinicius R, Acquaro Junior, Germán Augusto GomezRíos, Marcos Tascon and Queiroz Costa (2019). Analysis of endocannabinoids in plasma samples by biocompatible solid-phase microextraction devices coupled to mass spectrometry. Anal. Chim. Acta., 1091(73): 135-145.
Weihong Yin, Xiaojie Ju, Rui Xie, Wei Wang, Zhuang Liu and Liangyin Chu (2021). Dual drug-loaded coreshell microspheres for programmed sequential release. Chem. Eng. Prog., 40(2): 998-1007.
Wang Yan, MU Cong and Liu Jinfeng (2017). Effects of particle size of ticagrelor crude drug on in vivo dissolution behavior of ticagrelor tablet. China pharmacy. 28(1): 119-121.
Yadav M, Sarolia J, Vyas B, Lalan M, Mangrulkar S and Shah P (2021). Amalgamation of solid dispersion and melt adsorption technique: Improved In Vitro and In Vivo performance of ticagrelor tablets. AAPS Pharm. Sci. Tech., 22(8): 257.
Young-Guk Na, Jin-Ju Byeon, MiaoWang, Min-Ki Kim and Ki-Hyun Bang (2019). Statistical approach for solidifying ticagrelor loaded self-microemulsifying drug delivery system with enhanced dissolution and oral bioavailability. Mat. Sci. Eng. C., 104(27): 109980
Zhou L (2015). Construction of electrospinning sustainedrelease system with water-soluble drugs and Study on drug release. Su Zhou: Suzhou University.
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Published
Nov 25, 2023
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How to Cite
Ammara Farooq,Madeeha Anwar,Shahzaib khan,Saeed Ahmed Mirani, Hadia Farooq. (2023). Modeling of ticagrelor bioadhesive solid dispersion based on coaxial electrostatic spray to enhance oral bioavailability and improve drug release . Journal of Population Therapeutics and Clinical Pharmacology, 30(17), 702-712. https://doi.org/10.53555/jptcp.v30i17.3529
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All articles published in JPTCP are licensed under Copyright Creative Commons Attribution-NonCommercial 4.0 International License.
How to Cite
Ammara Farooq,Madeeha Anwar,Shahzaib khan,Saeed Ahmed Mirani, Hadia Farooq. (2023). Modeling of ticagrelor bioadhesive solid dispersion based on coaxial electrostatic spray to enhance oral bioavailability and improve drug release . Journal of Population Therapeutics and Clinical Pharmacology, 30(17), 702-712. https://doi.org/10.53555/jptcp.v30i17.3529