Peniche CJ, Peniche H, Bada N, Sáez V, Acosta N, PenicheI CA

Language: Spanish
References: 20
Page: 1-11
PDF size: 325.42 Kb.

ABSTRACT

Introduction: Parenteral administration systems based on in situ gelifying liquid formulations forming semi-solid implants for sustained drug release after injection, are very attractive for a number of reasons. Their application is less invasive and painful in comparison with solid implants, for the latter require local anesthesia and a minor surgical procedure. On the other hand, sustained systemic release of the drug may be achieved for prolonged periods.
Objective: Prepare a formulation for prolonged release of risperidone based on polymeric microparticles formed in situ. The system consists in an emulsion composed of a solution of a biodegradable polymer containing the drug (phase A) and an external oily stage (phase B). Microglobules in phase A solidify at the injection site, and the drug is released by the polymeric microparticles in a controlled manner.
Methods: The system used consisted in two syringes coupled by a connector to prepare the phase A emulsion in phase B. The phase B components evaluated were peanut, sesame and cottonseed oils. The polymer solvent used was N-Methyl-2- pyrrolidone. Two biodegradable polymers were tested as components of phase A: poly(D, L-lactide and poly(D, L-lactide-co-glycolide, to compare their influence on the release profile of risperidone.
Results: No important differences were found in the release profiles of risperidone when different oils were used in the oily phase. In the system prepared with poly(D, L-lactide), risperidone release is smaller after the first ten days of the assay, due to its greater hydrophobic nature and slower degradation rate in comparison with the poly(D, L-lactide-co-glycolide) system. With poly(D, L-lactide-co-glycolide) and peanut oil, a system was achieved which provided controlled release for 60 days.
Conclusions: Results show that this is a promising system for the development of a formulation for prolonged controlled release of risperidone.

REFERENCES

1. Niu CH, Chiu YY. FDA perspective on peptide formulation and stability issues. J Pharm Sci. 1998;87:1331.

2. Jain RA. The manufacturing techniques of varius drug loaded biodegradable poly(lactide-co-glycolide)(PLGA) devices. Biomaterials. 2000;21(23):2475-90.

3. Makadia HK, Siegel SJ. Poly lactic-co-glycolic acid (PLGA) as biodegradable controlled drug delivery carrier. Polymers (Basel). 2011;3:1377-97.

4. Jalil R, Nixon JR. Microencapsulation using poly(DL-lactic acid)II: Efect of polymer molecular weigth on the micrencapsule properties. Journal of Microencapsulation.7(2):245-54.

5. Versypt ANF. Mathematical modeling of drug delivery from autocatalytically degradable PLGA Microspheres - A review. The AAPS Journal. 2010;12:27-32.

6. Freitas S, Rudolf B, Merkle HP, Gander B. Flow-through ultrasonic emulsification combined with static micromixing for aseptic production of microspheres by solvent extraction. European Journal of Pharmaceutics and Biopharmaceutics. 2005;61:181-7.

7. Dhakar RC, Maurya SD, Saluja V. From Formulation Variables to Drug Entrapment Efficiency of Microspheres: A Technical Review. ournal of Drug Delivery & Therapeutics. 2012;2:128-33.

8. Bao W, Zhou J, Luo J, Wu D. PLGA microspheres with high drug loading and high encapsulation efficiency prepared by a novel solvent evaporation technique. Journal of Microencapsulation. 2006;23:471-9.

9. Bodmeier R. InventorVerfahren zur in-situ Herstellung von Partikeln. Offenlegungsschrift; 1997.

10. Kranz H, Bodmeier R. A biodegradable in situ forming system for controlled drug release. Pharm Sci Suppl. 1998;1:414.

11. Kranz H, Bodmeier R. A novel in situ forming drug delivery system for controlled parenteral drug delivery. Int J Pharm. 2007;332:107-14.

12. Jyothi NVN, Prasanna PM, Sakarkar SN, Prabha KS, Ramaiah PS, Srawan GY, et al. Microencapsulation techniques, factors influencing encapsulation efficiency. Journal of microencapsulation. 2010;27(3):187-97.

13. Prospecto del medicamento. 2016 [citado 17 de Nov de 2016]. Disponible en: http://wwwjanssencom/argentina/sites/www_janssen_com_argentina/files/product/p df/risperdal_constar-_ccds_feb2009_bipolar_set2010pdf

14. Anta L, Llaudó J, Ayani I, Gorostidi B, Monreal M, Martínez-González J, et al. Pharmacokinetics, safety, and tolerability of four 28-day cycle intramuscular injections for risperidone-ISM 75 mg in patients with schizophrenia: A phase-2 randomized study (PRISMA-2). 24th European Congress of Psychiatry / European Psychiatry. 2016;33S:S114-S289.

15. Su ZX, Shi YN, Teng LS, Li X, Wang LX, Meng QFl. Biodegradable poly(D, Llactide- co-glycolide) (PLGA) microspheres for sustained release of risperidone: Zeroorder release formulation. Pharmaceutical Development and Technology. 2011;16:377-84.

16. D'Souza S, Faraj JA, Giovagnoli S, DeLuca. PP. Development of Risperidone PLGA Microspheres. Journal of Drug Delivery. 2014;Article ID 620464.

17. An T, Choi J, Kim A, Lee JH, Nam Y, Park J, et al. Sustained release of risperidone from biodegradable microspheres prepared by in-situ suspension-evaporation process. International Journal of Pharmaceutics. 2016 [citado 13 de octubre de 2016]. Disponible en: https://doi.org/10.1016/j.ijpharm.2016.02.023

18. Yapar EA, İnal Ö, Özkan Y, Baykara T. Injectable In Situ Forming Microparticles: A Novel Drug Delivery System.. Tropical Journal of Pharmaceutical Research. 2012;11:307-18.

19. Su ZX, Shi YN, Teng LS, Li X, Wang LX, Meng QF, et al. Biodegradable poly(D, Llactide- co-glycolide) (PLGA) microspheres for sustained release of risperidone: Zeroorder release formulation Pharmaceutical Development and Technology. 2011;16:377-84.

20. An T, Choi J, Kim A, Lee J, Ho N, Yoonjin P, et al. Sustained release of risperidone from biodegradable microspheres prepared by in-situ suspension-evaporation process. International Journal of Pharmaceutics. 2016 [citado 3 de junio de 2016]. Disponible en: http://dx.doi.org/10.1016/j.ijpharm.2016.02.023