Development and characterization of lyophilized diazepam-loaded polymeric micelles

AAPS PharmSciTech

Volumn 15, Issue 1, 2014, Pages 52-64

  Suksiriworapong, Jiraphong ^a   Rungvimolsin, Tanaporn ^a   A Gomol, Atitaya ^a   Junyaprasert, Varaporn Buraphacheep ^a   Chantasart, Doungdaw ^a  

^a MAHIDOL UNIVERSITY   (Thailand)

Author keywords

d tocopheryl poly(ethylene glycol) 1000 succinate (TPGS); diazepam; lyophilization; poloxamer 407; polymeric micelles

Indexed keywords

DIAZEPAM; DRUG CARRIERS; DRUG STABILITY; FREEZE DRYING; MICELLES; PARTICLE SIZE; POLOXAMER; POLYETHYLENE GLYCOLS; POLYMERS; POWDERS;

EID: 84893704496     PISSN: None     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/s12249-013-0032-4     Document Type: Article

References (43)

1. Milligan NM, Dhillon S, Griffiths A, Oxley J, Richens A. A clinical trial of single dose rectal and oral administration of diazepam for the prevention of serial seizures in adult epileptic patients. J Neurol Neurosurg Psychiatry. 1984;47(3):235-40.
2. Taketomo CK, Hodding JH, Kraus DM. Pediatric & neonatal dosage handbook with international trade names index. 18th ed. Ohio: Lexi-Comp, Inc.; 2011-2012.
3. Hirabayashi Y, Okumura A, Kondo T, Magota M, Kawabe S, Kando N, et al. Efficacy of a diazepam suppository at preventing febrile seizure recurrence during a single febrile illness. Brain Dev. 2009;31(6):414-8.
4. Otsuka H, Nagasaki Y, Kataoka K. Self-assembly of poly(ethylene glycol)-based block copolymers for biomedical applications. Curr Opin Colloid Interface Sci. 2001;6(1):3-10.
5. Miyata K, Christie RJ, Kataoka K. Polymeric micelles for nano-scale drug delivery. React Funct Polym. 2011;71(3):227-34.
6. Aliabadi HM, Lavasanifar A. Polymeric micelles for drug delivery. Expert Opin Drug Deliv. 2006;3(1):139-62.
7. Gao Z, Eisenberg A. A model of micellization for block copolymers in solutions. Macromolecules. 1993;26(26):7353-60.
8. Yamamoto T, Yokoyama M, Opanasopit P, Hayama A, Kawano K, Maitani Y. What are determining factors for stable drug incorporation into polymeric micelle carriers? Consideration on physical and chemical characters of the micelle inner core. J Control Release. 2007;123(1):11-8.
9. Hoffman NE, Hofmann AF. A comparison of the rate of absorption micellar and nonmicellar oleic acid. A jejunal perfusion study in man. Am J Dig Dis. 1973;18(6):489-92.
10. Woollett LA, Wang Y, Buckley DD, Yao L, Chin S, Granholm N, et al. Micellar solubilisation of cholesterol is essential for absorption in humans. Gut. 2006;55(2):197-204.
11. Watt SM, Simmonds WJ. The specificity of bile salts in the intestinal absorption of micellar cholesterol in the rat. Clin Exp Pharmacol Physiol. 1976;3(4):305-22.
12. Lavasanifar A, Samuel J, Kwon GS. The effect of fatty acid substitution on the in vitro release of amphotericin B from micelles composed of poly(ethylene oxide)-block-poly(N-hexyl stearate-l-aspartamide). J Control Release. 2002;79(1-3):165-72.
13. Aliabadi HM, Mahmud A, Sharifabadi AD, Lavasanifar A. Micelles of methoxy poly(ethylene oxide)-b-poly(epsilon-caprolactone) as vehicles for the solubilization and controlled delivery of cyclosporine A. J Control Release. 2005;104(2):301-11.
14. Nishiyama N, Okazaki S, Cabral H, Miyamoto M, Kato Y, Sugiyama Y, et al. Novel cisplatin-incorporated polymeric micelles can eradicate solid tumors in mice. Cancer Res. 2003;63(24):8977-83.
15. Ashok B, Arleth L, Hjelm RP, Rubinstein I, Onyuksel H. In vitro characterization of PEGylated phospholipid micelles for improved drug solubilization: effects of PEG chain length and PC incorporation. J Pharm Sci. 2004;93(10):2476-87.
16. Rupp C, Steckel H, Muller BW. Solubilization of poorly water-soluble drugs by mixed micelles based on hydrogenated phosphatidylcholine. Int J Pharm. 2010;395(1-2):272-80.
17. Schmolka I. A review of block polymer surfactants. J Am Oil Chem Soc. 1977;54(3):110-6.
18. Kabanov AV, Batrakova EV, Miller DW. Pluronic block copolymers as modulators of drug efflux transporter activity in the blood-brain barrier. Adv Drug Deliv Rev. 2003;55(1):151-64.
19. Kabanov AV, Batrakova EV, Alakhov VY. Pluronic® block copolymers as novel polymer therapeutics for drug and gene delivery. J Control Release. 2002;82(2-3):189-212.
20. Mu L, Feng SS. Vitamin E TPGS used as emulsifier in the solvent evaporation/extraction technique for fabrication of polymeric nanospheres for controlled release of paclitaxel (Taxol). J Control Release. 2002;80(1-3):129-44.
21. Krasavage WJ, Terhaar CJ. d-alpha-Tocopheryl poly(ethylene glycol) 1000 succinate. Acute toxicity, subchronic feeding, reproduction, and teratologic studies in the rat. J Agric Food Chem. 1977;25(2):273-8.
22. Mu L, Elbayoumi TA, Torchilin VP. Mixed micelles made of poly(ethylene glycol)-phosphatidylethanolamine conjugate and d-alpha-tocopheryl polyethylene glycol 1000 succinate as pharmaceutical nanocarriers for camptothecin. Int J Pharm. 2005;306(1-2):142-9.
23. Moynihan H, Crean A. The theory of disperse systems. In: Moynihan H, Crean A, editors. The physicochemical basis of pharmaceuticals. New York: Oxford University Press Inc.; 2009. p. 156-92.
24. 2-poly(ethylene glycol) nanoparticles with grafting nicotinic acid as drug carriers. Int J Pharm. 2012;423(2):562-70.
25. The United State Pharmacopeia Convention. The United States Pharmacopeia (USP) 35/The National Formulary (NF) 30. Baltimore: United Book Press, Inc.; 2012.
26. Anhorn MG, Mahler HC, Langer K. Freeze drying of human serum albumin (HSA) nanoparticles with different excipients. Int J Pharm. 2008;363(1-2):162-9.
27. Holzer M, Vogel V, Mantele W, Schwartz D, Haase W, Langer K. Physico-chemical characterisation of PLGA nanoparticles after freeze-drying and storage. Eur J Pharm Biopharm. 2009;72(2):428-37.
28. Kamal BA. The release of diazepam from different conventional and hollow type suppository bases. Iraqi J Pharm Sci. 2007;16(2):21-6.
29. Kaewnopparat N, Oungpho K, Kaewnopparat S, Rittirod T, Rojanarat W, Tessiri T. Preparation of extemporaneously diazepam suppositories: in vitro release and aging study. IJPS. 2006;2(1):26-34.
30. Siepmann J, Peppas NA. Modeling of drug release from delivery systems based on hydroxypropyl methylcellulose (HPMC). Adv Drug Deliv Rev. 2001;48(2-3):139-57.
31. AydIn RST, Pulat M. 5-Fluorouracil encapsulated chitosan nanoparticles for pH-stimulated drug delivery: evaluation of controlled release kinetics. J Nanomater. 2012;2012(313961):10.
32. Dash S, Murthy PN, Nath L, Chowdhury P. Kinetic modeling on drug release from controlled drug delivery systems. Acta Pol Pharm. 2010;67(3):217-23.
33. Costa P, Sousa Lobo JM. Modeling and comparison of dissolution profiles. Eur J Pharm Sci. 2001;13(2):123-33.
34. Serra L, Doménech J, Peppas NA. Drug transport mechanisms and release kinetics from molecularly designed poly(acrylic acid-g-ethylene glycol) hydrogels. Biomaterials. 2006;27(31):5440-51.
35. Guidance for industry: Dissolution testing of immediate release solid oral dosage forms [database on the Internet]. U.S. Department of Health and Human Services Food and Drug Administration Center for Drug Evaluation and Research (CDER). 1997 [cited September 1, 2011]. Available from: http://www.fda.gov/cder/guidance/1713bp1.pdf.
36. Wickersham RM, Novak KK. Drug facts and comparisons. 2012th ed. St. Louis: Kluwer; 2012.
37. Sezgin Z, Yüksel N, Baykara T. Preparation and characterization of polymeric micelles for solubilization of poorly soluble anticancer drugs. Eur J Pharm Biopharm. 2006;64(3):261-8.
38. Yu L, Bridgers A, Polli J, Vickers A, Long S, Roy A, et al. Vitamin E-TPGS increases absorption flux of an HIV protease inhibitor by enhancing its solubility and permeability. Pharm Res. 1999;16(12):1812-7.
39. Ismailos G, Reppas C, Macheras P. Enhancement of cyclosporin A solubility by d-alphatocopheryl-polyethylene-glycol-1000 succinate (TPGS). Eur J Pharm Sci. 1994;1(5):269-71.
40. Alexandridis P, Alan Hatton T. Poly(ethylene oxide)-poly(propylene oxide)-poly(ethylene oxide) block copolymer surfactants in aqueous solutions and at interfaces: thermodynamics, structure, dynamics, and modeling. Colloids Surf Physicochem Eng Aspects. 1995;96(1-2):1-46.
41. Brown W, Schillen K, Almgren M, Hvidt S, Bahadur P. Micelle and gel formation in a poly(ethylene oxide)/poly(propylene oxide)/poly(ethylene oxide) triblock copolymer in water solution: dynamic and static light scattering and oscillatory shear measurements. J Phys Chem. 1991;95(4):1850-8.
42. Abdelbary AA, Li X, El-Nabarawi M, Elassasy A, Jasti B. Effect of fixed aqueous layer thickness of polymeric stabilizers on zeta potential and stability of aripiprazole nanosuspensions. Pharm Dev Technol. 2013;18(3):730-5.
43. Keck CM. Cyclosporine nanosuspensions: optimised size characterisation & oral formulations. Berlin: Freie Universität; 2006.