Formulation and In Vivo Evaluation of Ticagrelor Self-nanoemulsifying Drug Delivery Systems. 2021

Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
Mewar University, Chittorgarh-312901, Rajasthan, India.

Ticagrelor (TGR), being an antiplatelet agent, belongs to BCS class IV drug with low solubility and permeability that undergoes first-pass metabolism, leading to reduced bioavailability of 36%. The main objective of this study is to develop TGR SNEDDS for enhancing solubility and oral bioavailability. An oil, surfactant and co-surfactant (miglyol 810, brij 35 and lauro glycol FCC) are chosen based on the maximum solubility of TGR. The selected vehicles are mixed in different ratios and are agitated mildly. Transmittance values that are more than 80 were noted and are used for constructing pseudo ternary phase diagram. Formulations that passed stability testing were evaluated for % transmission, drug content and in vitro drug release analysis. In vivo bioavailability studies of optimized SNEDDS are performed in Wistar rats. From evaluation studies of TGR, formulation F13 with maximum drug release of 98.99% in 60 minutes, that is higher than 31.99% of the pure drug is considered as an optimised formulation. The particle size, Z average and zeta potential of the optimized TGR formulation F13 was 289.6 nm, 185.1 nm and -18.3 mV respectively. The FTIR and SEM studies do not indicate any drug excipient interaction and confirm nano size which is stable for 3 months. From in vivo bioavailability studies in rats, the Cmax of optimized TGR SNEDDS (302.43±4.78 ng/ml) is higher than pure TGR suspension (47.32±2.75 ng/ml) and optimized SNEDDS exhibited 5 folds increase in oral bioavailability when compared to pure drug. Hence the results reveal that, application of SNEDDS formulation technique for TGR Increases solubility and oral bioavailability.

UI MeSH Term Description Entries
D004655 Emulsions Colloids formed by the combination of two immiscible liquids such as oil and water. Lipid-in-water emulsions are usually liquid, like milk or lotion. Water-in-lipid emulsions tend to be creams. The formation of emulsions may be aided by amphiphatic molecules that surround one component of the system to form MICELLES. Emulsion
D000077486 Ticagrelor An adenosine triphosphate analogue and reversible P2Y12 PURINORECEPTOR antagonist that inhibits ADP-mediated PLATELET AGGREGATION. It is used for the prevention of THROMBOEMBOLISM by patients with ACUTE CORONARY SYNDROME or a history of MYOCARDIAL INFARCTION. 3-(7-((2-(3,4-Difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-(1-3)-triazolo(4,5-d)pyrimidin-3-yl)-5-(2-hydroxyethoxy)cyclopentane-1,2-diol,AZD 6140,AZD-6140,AZD6140,Brilinta,Brilique
D000284 Administration, Oral The giving of drugs, chemicals, or other substances by mouth. Drug Administration, Oral,Administration, Oral Drug,Oral Administration,Oral Drug Administration,Administrations, Oral,Administrations, Oral Drug,Drug Administrations, Oral,Oral Administrations,Oral Drug Administrations
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D016503 Drug Delivery Systems Systems for the delivery of drugs to target sites of pharmacological actions. Technologies employed include those concerning drug preparation, route of administration, site targeting, metabolism, and toxicity. Drug Targeting,Delivery System, Drug,Delivery Systems, Drug,Drug Delivery System,Drug Targetings,System, Drug Delivery,Systems, Drug Delivery,Targeting, Drug,Targetings, Drug
D017208 Rats, Wistar A strain of albino rat developed at the Wistar Institute that has spread widely at other institutions. This has markedly diluted the original strain. Wistar Rat,Rat, Wistar,Wistar Rats
D051381 Rats The common name for the genus Rattus. Rattus,Rats, Laboratory,Rats, Norway,Rattus norvegicus,Laboratory Rat,Laboratory Rats,Norway Rat,Norway Rats,Rat,Rat, Laboratory,Rat, Norway,norvegicus, Rattus

Related Publications

Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
December 2017, Colloids and surfaces. B, Biointerfaces,
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
January 2019, International journal of pharmaceutics,
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
December 2010, Nanomedicine (London, England),
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
November 2017, European journal of pharmaceutical sciences : official journal of the European Federation for Pharmaceutical Sciences,
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
April 2016, International journal of pharmaceutics,
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
January 2022, Pharmaceutics,
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
October 2008, International journal of pharmaceutics,
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
April 2020, International journal of pharmaceutics,
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
January 2021, Journal of pharmacy & bioallied sciences,
Adella Aparna, and Yamsani Shravan Kumar, and Darna V R N Bhikshapathi
October 2012, Expert opinion on drug delivery,
Copied contents to your clipboard!