International Journal of Nanomedicine (Jun 2022)

Cefquinome Sulfate Oily Nanosuspension Designed for Improving its Bioavailability in the Treatment of Veterinary Infections

  • Mao Y,
  • Chen Y,
  • Liu C,
  • He X,
  • Zheng Y,
  • Chen X,
  • Wang Y,
  • Chen W,
  • Wu Y,
  • Shen Y,
  • Yang H,
  • Ma S

Journal volume & issue
Vol. Volume 17
pp. 2535 – 2553

Abstract

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Yujuan Mao,1 Yumeng Chen,2 Chang Liu,2 Xingyue He,2 Yi Zheng,1 Xiaolan Chen,1 Ying Wang,1 Wei Chen,1 Yanling Wu,1 Yan Shen,2 Haifeng Yang,1 Songbo Ma3 1Jiangsu Animal Husbandry and Veterinary College, Taizhou, Jiangsu, 225300, People’s Republic of China; 2State Key Laboratory of Natural Medicines, Center for Research Development and Evaluation of Pharmaceutical Excipients and Generic Drugs, Department of Pharmaceutics, School of Pharmacy, China Pharmaceutical University, Nanjing, People’s Republic of China; 3Department of Oral and Maxillofacial Surgery, Taizhou People’s Hospital, Taizhou, Jiangsu, 225300, People’s Republic of ChinaCorrespondence: Haifeng Yang, Email [email protected]; Songbo Ma, Email [email protected]: Cefquinome sulfate (CS) is the first fourth-generation antibiotic for animals, which has a wide antibacterial spectrum, strong antibacterial activity and low drug resistance. However, it is accompanied by problems of poor therapeutic efficacy. In this context, the use of nanosuspensions have been found to be an attractive strategy. The main objective of this work is to develop a new oily nanosuspension to improve bioavailability and stability of CS formulations.Methods: After screening the formulations, cefquinome sulfate oily nanosuspension (CS-NSP) was prepared by mortar grinding, using propylene glycol dicaprolate/dicaprate (Labrafac™ PG) as oil medium and caprylocaproyl polyoxyl-8 glycerides (Labrasol®) as stabilizer. The properties of CS-NSP were investigated by testing its physicochemical characteristics, stability, in vitro release, hemolysis, and muscle irritation. The in vivo pharmacokinetics of CS-NSP was studied using rats.Results: Results show that CS-NSP presents suitable stability, physicochemical properties and safety. Moreover, a rapid release and high bioavailability of CS-NSP have also been verified in the study. Pharmacokinetic experiments in vivo showed that the bioavailability of CS-NSP was about 1.6 times that of commercial cefquinome sulfate injection (CS-INJ, Chuangdao®) (p< 0.01). These advantages of CS-NSP were carried out by small particle size and low viscosity, being associated with the use of Labrafac PG and stabilizer Labrasol.Conclusion: The results proved that the new preparation is safe and effective and is expected to become a promising veterinary nanodelivery system.Keywords: cefquinome sulfate, oily nanosuspension, Labrafac PG, labrasol, pharmacokinetics

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