Formulation and performance characterization of radio-sterilized "Progestin-only" microparticles intended for contraception

AAPS PharmSciTech

Volumn 10, Issue 2, 2009, Pages 443-452

  Puthli, Shivanand ^a   Vavia, Pradeep ^a  

^a INSTITUTE OF CHEMICAL TECHNOLOGY   (India)

Author keywords

Contraceptive; Gamma radiation; In vivo; Levonorgestrel; Poly(lactide co glycolide)

Indexed keywords

LEVONORGESTREL; METHYLCELLULOSE; MICROSPHERE; POLYGLACTIN; POLYVINYL ALCOHOL; CONTRACEPTIVE AGENT; LACTIC ACID; POLYGLYCOLIC ACID; POLYLACTIC ACID POLYGLYCOLIC ACID COPOLYMER; POLYLACTIC ACID-POLYGLYCOLIC ACID COPOLYMER;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTRACEPTION; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG BLOOD LEVEL; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; FEMALE; FEMALE STERILITY; GAMMA RADIATION; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; IN VITRO STUDY; IN VIVO STUDY; INFRARED SPECTROSCOPY; MICROEMULSION; MICROENCAPSULATION; MOISTURE; NONHUMAN; PARTICLE SIZE; RABBIT; RADIATION STERILIZATION; X RAY DIFFRACTION; ANIMAL; CHEMISTRY; INFRARED SPECTROPHOTOMETRY; INSTRUMENT STERILIZATION; SCANNING ELECTRON MICROSCOPY; SOLUBILITY;

ANIMALS; AREA UNDER CURVE; CALORIMETRY, DIFFERENTIAL SCANNING; CHEMISTRY, PHARMACEUTICAL; CONTRACEPTIVE AGENTS, FEMALE; FEMALE; GAMMA RAYS; LACTIC ACID; LEVONORGESTREL; MICROSCOPY, ELECTRON, SCANNING; MICROSPHERES; POLYGLYCOLIC ACID; RABBITS; SOLUBILITY; SPECTROPHOTOMETRY, INFRARED; STERILIZATION; X-RAY DIFFRACTION;

EID: 67549105384     PISSN: None     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/s12249-009-9226-1     Document Type: Article

References (35)

1. Jiang W, Gupta RK, Deshpande MC, Schwendeman SP. Biodegradable poly(lactide-co-glycolide) microparticles for injectable delivery of vaccine antigens. Adv Drug Deliv Rev 2005;57:391-410.
2. Panyam J, Labhasetwar V. Biodegradable nanoparticles for drug and gene delivery to cells and tissues. Adv Drug Deliv Rev 2003;55:329-47.
3. Mundargi RC, Ramesh Babu V, Rangaswamy V, Patel P, Aminabhavi TM. Nano/ micro technologies for delivering macromolecular therapeutics using poly(D,L-lactide-co-glycolide) and its derivatives. J Control Release 2008;125:193-209.
4. Heya T, Okada H, Ogawa Y, Toguchi H. Factors influencing the profiles of TRH release from copoly(d,l-lactic/glycolic acid) microspheres. Int J Pharm 1991;72:199-205.
5. Sah HK, Chien YW. Evaluation of a microreservoir-type biodegradable microcapsule for controlled release of proteins. Drug Dev Ind Pharm 1993;19:1243-63.
6. Urata T, Arimori K, Nakano M. Modification of release rates of cyclosporin A from polyl(L-lactic acid) microspheres by fatty acid esters and in-vivo evaluation of the microspheres. J Control Release 1999;58:133-41.
7. Chattaraj SC, Rathinavelu A, Das SK. Biodegradable microparticles of influenza viral vaccine: Comparison of the effects of routes of administration on the in vivo immune response in mice. J Control Release 1999;58:223-32.
8. Viswanathan NB, Thomas PA, Pandit JK, Kulkarni MG, Mashelkar RA. Preparation of non-porous microspheres with high entrapment efficiency of proteins by a (water-in-oil)-in-oil emulsion technique. J. Control Release 1999;58:9-20.
9. Okada HY, Heya IT, Uneo H, Ogawa Y, Toguchi H. Pharmacokinetics of once-a-month injectable microspheres of leuprolide acetate. Pharm Res 1991;8:787-91.
10. Wang SH, Zhang LC, Lin F, Sa XY, Zuo JB, Shao QX, Chen GS, Zeng S. Controlled release of levonorgestrel from biodegradable poly(d,l-lactide-co-glycolide) microspheres: In vitro and in vivo studies. Int J Pharm 2005;301:217-25.
11. Beck LR, Pope VZ, Tice TR, Gilley RM. Long-acting injectable microsphere formulation for the parenteral administration of levonorgestrel. Adv Contracept 1985;1:119-29.
12. Lovgren K, Lundberg P. Determination of sphericity of pellets prepared by extrusion/spheronization and the impact of some process parameters. Drug Dev Ind Pharm 1989;15:2375-92.
13. Higuchi T. Mechanism of sustained action medication: Theoretical analysis of rate of release of solid drugs dispersed in solid matrices. J Pharm Sci 1963;52:1145-9.
14. Doshi CC, Bhalla HL. In vitro release studies of levonorgestrel loaded biodegradable microspheres. Ind J Pharm Sci 1999;61:39-43.
15. Shah MV, De Gennaro MD, Suryakasuma H. An evaluation of albumin microcapsules prepared using a multiple emulsion technique. J Microencapsul 1987;4:223-38.
16. Ranga Rao KV, Padmalatha DK, Buri PK. Cellulose matrices for zero-order release of soluble drugs. Drug Dev Ind Pharm 1988;14:2299-320.
17. United States Pharmacopoeia, Microbiological tests: Sterility Tests, USP 29-NF 24, The United States Pharmacopoeial Convention, Inc., Rockville, 2006.
18. European Pharmacopoeia, Appendix XIVD Test for pyrogens, Ph. Eur. method 2.6.8, Council of Europe, 2005.
19. Beck LR, Pope VZ. Controlled-release delivery systems for hormones. A review of their properties and current therapeutic use. Drugs 1984;27:528-47.
20. Sanders LM, Kent JS, McRae GI, Vickery BH, Tice TR, Lewis DH. Controlled release of a luteinizing hormone-releasing hormone analogue from poly(d,l-lactide-co-glycolide) microspheres. J Pharm Sci 1984;73:1294-7.
21. Spenlehauer G, Vert M, Benoit JP, Chabot F, Veillard M. Biodegradable cisplatin microspheres prepared by the solvent evaporation method: morphology and release characteristics. J Control Release 1988;7:217-29.
22. Spenlehauer G, Vert M, Benoit JP, Boddaert A. In vitro and in vivo degradation of poly(D,L lactide/glycolide) type microspheres made by solvent evaporation method. Biomaterials 1989;10:557-63.
23. Ruiz JM, Busnel JP, Benoit JP. Influence of average molecular weights of poly(DL-lactic acid-co-glycolic acid) copolymers 50/50 on phase separation and in vitro drug release from microspheres. Pharm Res 1990;7:928-34.
24. Wise DL, Trantolo DJ, Marino RT, Kitchell JP. Opportunities and challenges in the design of implantable biodegradable polymeric systems for the delivery of antimicrobial agents and vaccines. Adv Drug Deliv Rev 1987;1:19-39.
25. Hartas SR, Collett JH, Booth C. The influence of gamma-irradiation on the release of melatonin from poly(lactide-coglycolide) microspheres. Proc Int Symp Control Release Bioact Mater 1992;19:321-2.
26. Crossan IM, Whateley TL. Microspheres of dexamethasone as a biodegradable controlled release drug delivery system. Proc Int Symp Control Release Bioact Mater 1994;21:184-5.
27. Fallon PA, Whateley TL. The development and evaluation of poly(lactic-glycolic acid) implants for sustained delivery of dexamethasone to the brain. Proc Int Symp Control Release Bioact Mater 1994;21:264-5.
28. Yoshioka S, Aso Y, Otsuka T, Kojima S. The effect of γ-irradiation on drug release from poly(lactide) microspheres. Radiat Phys Chem 1995;46:281-5.
29. ICH harmonized tripartite guideline, Q3C(R3) Impurities: Guideline for residual solvents (http://www.ich.org/lob/media/media423.pdf).
30. Roy S, Stanczyk FZ, Mishell DR, Lumkin M, Gentzschein E. Clinical and endocrinologic study of continuous levonorgestrel administration from subcutaneous solid polydimethylsiloxane rods. Contraception 1980;21:595-615.
31. Moore DE, Roy S, Stanczyk FZ, Mishell D. Bleeding and serum d-norgestrel, estradiol and progesterone patterns in women using d-norgestrel subdermal polysiloxane capsules for contraception. Contraception 1978;17:315-28.
32. Ory SJ, Hammond CB, Yancy SG, Hendren RW, Pitt CG. The effect of a biodegradable contraceptive capsule (Capronor) containing levonorgestrel on gonadotropin, estrogen, and progesterone levels. Am J Obstet Gynecol 1983;145:600-5.
33. Sivin I, Lähteenmäki P, Ranta S, Darney P, Klaisle C, Wan L, Mishell DR, Lacarra M, Viegas OA, Bilhareus P, Koetsawang S, Piya-Anant M, Diaz S, Pavez M, Alvarez F, Brache V, LaGuardia K, Nash H, Stern J. Levonorgestrel concentrations during use of levonorgestrel rod (LNG ROD) implants. Contraception 1997;55:81-5.
34. Lancranjan I, Bruns C, Grass P, Jaquet P, Jervell J, Kendall-Taylor P, Lamberts SW, Marbach P, Orskov H, Pagani G, Sheppard M, Simionescu L. Sandostatin LAR: A promising therapeutic tool in the management of acromegalic patients. Metabolism 1996;45:67-71.
35. Comets E, Mentre F, Kawai R, Nimmerfall F, Marbach P, Vonderscher J. Modeling the kinetics of release of octreotide from long-acting formulations injected intramuscularly in rabbits. J Pharm Sci 2000;89:1123-33.