ALTERATION OF PHARMACOKINETIC PARAMETERS OF PENTOXIFYLLINE USING NATURAL MUCOADHESIVE POLYMERS

  • GNANASEKARAN JOHN SELVARAJ Department of Pharmacy Practice, Vinayaka Mission’s College of Pharmacy, Vinayaka Mission’s Research Foundation (Deemed to be University), Salem 636008, Tamilnadu, India
  • ARUL BALASUBRAMANIAN Department of Pharmacy Practice, Vinayaka Mission’s College of Pharmacy, Vinayaka Mission’s Research Foundation (Deemed to be University), Salem 636008, Tamilnadu, India
  • KOTHAI RAMALINGAM Department of Pharmacy Practice, Vinayaka Mission’s College of Pharmacy, Vinayaka Mission’s Research Foundation (Deemed to be University), Salem 636008, Tamilnadu, India

Abstract

Objective: The present study was aimed to alter the pharmacokinetic parameters of the drug pentoxifylline using a novel natural mucoadhesive polymer from two different plants, Manilkara zapotta Linn and Ocimum basilicum Linn.


Methods: The polymer was isolated and six batches of mucoadhesive tablets of pentoxifylline was formulated with 3 different concentrations of each polymer. The best formulation from each of the polymer was selected and administered to rabbits and the plasma drug concentration was compared with the marketed formulation. The pharmacokinetic parameters such as such as Cmax, tmax, AUC, AUMC, λz, t1/2, and MRT were determined.


Results: The plasma drug concentration vs time curve shows the extended-release of pentoxifylline when compared with the conventional marketed formulation. The results show that there is no change in the peak plasma concentration, but the significant difference was observed in t½, which showed approximately 2.5 fold increase from 2.44 to 6.87 h and the AUC showed five-fold increase from 22.40 to 117.19 μg*h/ml, and other pharmacokinetic parameters, when compared with the marketed formulation.


Conclusion: The isolated polymer from the plants Manilkara zapotta Linn. and Ocimum basilicum Linn can be used as a carrier for developing mucoadhesive formulations and it alter the pharmacokinetic of pentoxifylline positively.

Keywords: Mucoadhesion, Manilkara zapotta, Ocimum basilicum, Pentoxifylline, Pharmacokinetics

References

1. Jimenez Castellanos MR, Zia H, Rhodes CT. Mucoadhesive drug delivery systems. Drug Dev Ind Pharm 1993;19:143–94.
2. Ahuja A, Khar RK, Ali J. Mucoadhesive drug delivery systems. Drug Dev Ind Pharm 1997;23:489–515.
3. Nagai T MY. Advances in drug delivery, mucosal adhesive dosage forms. Pharm Int 1985;6:196–200.
4. Gayot A. Bioadhesive polymers. J Pharm Belg 1985;40:332–8.
5. Shin SC, Kim JY. Enhanced permeation of triamcinolone acetonide through the buccal mucosa. Eur J Pharm Biopharm 2000;50:217–20.
6. Cilurzo F, Minghetti P, Selmin F, Casiraghi A, Montanari L. Polymethacrylate salts as new low-swellable mucoadhesive materials. J Controlled Release 2003;88:43–53.
7. Han Gon C, Jac Hee J, Chul Soon Y, Chong Dal R, Mi Kyung L, Jeong Hee H, Kyung-mi P C-KK. Formulation and in vitro evaluation of omeperazole buccal adhesive tablet. J Controlled Release 2000;68:405–12.
8. Miyazaki S, Kawasaki N, Nakamura T, Iwatsu M, Hou WM, Attwood D. Oral mucosal bioadhesive tablets of pectin and HPMC: in vitro and in vivo evaluation. Int J Pharm 2000;204:127–32.
9. Shah HP, Prajapati ST, Patel C. Gastroretentive drug delivery systems: from conception to commercial success. J Crit Rev 2017;4:10–21.
10. Ward A, Clissold SP. Pentoxifylline. A review of its pharmacodynamic and pharmacokinetic properties, and its therapeutic efficacy. Drugs 1987;34:50–97.
11. Beermann B, Ings R, Mansby J, Chamberlain J, McDonald A. Kinetics of intravenous and oral pentoxifylline in healthy subjects. Clin Pharmacol Ther 1985;37:25–8.
12. Morais PLD, Miranda MRA, Lima LCO, Alves JD, Alves RE, Silva JD. Cell wall biochemistry of sapodilla (Manilkara zapota) submitted to 1-methylcyclopropene. Brazilian J Plant Physiol 2008;20:85–94.
13. Osman MA, Rashid MM, Aziz MA, Habib MR, Karim MR. Inhibition of ehrlich ascites carcinoma by Manilkara zapota L. stem bark in swiss albino mice. Asian Pac J Trop Biomed 2011;1:448–51.
14. Chanda SV NK. Antioxidant capacity of Manilkara zapota L. leaves extracts evaluated by four in vitro methods. Nat Sci 2010;8:260–6.
15. Nair R, Chanda S. Antimicrobial activity of Terminalia catappa, Manilkara zapota and Piper betel leaf extract. Indian J Pharm Sci 2008;70:390–3.
16. Kaneria M, Baravalia Y, Vaghasiya Y, Chanda S. Determination of antibacterial and antioxidant potential of some medicinal plants from saurashtra region, India. Indian J Pharm Sci 2009;71:406–12.
17. Sudarshan Singh, Sunil B Bothara. Manilkara zapota (Linn.) seeds: a potential source of natural gum. ISRN Pharm 2014:1–10.
18. Prakash V. Leafy spices. CRC Press; 1990. p. 114.
19. Simon J, Quinn J, Murray R. Basil: a source of essential oil. In: Advances in new crops. J Janick, Simon J. editors. Timloer Press: Portland OR; 1990. p. 484–9.
20. Marotti M, Piccaglia R, Giovanelli E. Differences in essential oil composition of basil (Ocimum basilicum L.) Italian cultivars related to morphological characteristics. J Agric Food Chem 1996;44:3926–9.
21. Mathews S, Singhal RS, Kulkarni PR. Ocimum basilicum: a new non-conventional source of fibre. Food Chem 1993;47:399–401.
22. Gnanasekaran J, Arul B, Kothai R. Development of mucoadhesive tablet of pentoxifylline using a natural polymer from Manilkara zapota linn. Int J Appl Pharm 2019;11:88–91.
23. Balasubramanian A, John Selvaraj G, Ramalingam K. Application of novel natural mucoadhesive polymer in the development of pentoxifylline mucoadhesive tablets. Int J Appl Pharm 2019;11:37-41.
24. Rao PS SH. Tamarind. In: Industrial Gums. 2nd edn. RL W. editor. Academic Press, New York; 1973. p. 369–411.
25. Yan KS, Yan TX, Guo H, Li JZ, Wei LL, Wang C. Evaluation of transdermal permeability of pentoxifylline gel: in vitro skin permeation and in vivo microdialysis using wistar rats. Drug Discovery Ther 2007;1:78–83.
26. Teksin ZS, Agabeyoglu I, Yamac K. Bioavailability of pentoxifylline-chitosan. J Bioequiv Available 2009;1:115–20.
27. Hussein AH. Formulation and evaluation of sustained release tablets of pentoxifylline using okra extract as a novel retardant. Int J Pharm Pharm Sci 2014;7:204–8.
28. Saikia T, Ali J, Das B. Isolation and characterization of tamarind seed polysaccharide-a natural lrease retardant. Int J Curr Pharm Res 2017;9:114–7.
29. Pandey S, Shah RR, Gupta A, Arul B. Design and evaluation of buccoadhesive controlled release formulations of prochlorperazine maleate. Int J Pharm Pharm Sci 2016;8:375–9.
30. Nishad K, Arul B, Rajasekaran S. Design and comparative evaluation of clarithromycin gastric bioadhesive tablets by ex-vivo and in vivo methods. Asian J Pharm Clin Res 2018;11:248–56.
31. Harris D, Fell JT, Taylor DC, Lynch J, Sharma HL. GI transit of potential bioadhesive systems in the rat. J Controlled Release 1990;12:55–65.
32. Smith RV, Waller ES, Doluisio JT, Bauza MT, Puri SK, Ho I. Pharmacokinetics of orally administered pentoxifylline in humans. J Pharm Sci 1986;75:47–52.
33. Mauro VF, Mauro LS, Hageman JH. Alteration of pentoxifylline pharmacokinetics by cimetidine. J Clin Pharmacol 1988;28: 649–54.
34. Antignani PL, Todini AR, Saliceti F, Pacino G, Bartolo M. Results of clinical, laboratory and haemorheological investigations of the use of pentoxifylline in high doses. Pharmatherapeutica 1987;5:50–6.
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SELVARAJ, G. J., BALASUBRAMANIAN, A., & RAMALINGAM, K. (2019). ALTERATION OF PHARMACOKINETIC PARAMETERS OF PENTOXIFYLLINE USING NATURAL MUCOADHESIVE POLYMERS. International Journal of Applied Pharmaceutics, 12(1), 153-157. https://doi.org/10.22159/ijap.2020v12i1.36080
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