Chitosan based atorvastatin nanocrystals: Effect of cationic charge on particle size, formulation stability, and in-vivo efficacy

International Journal of Nanomedicine

Volumn 10, Issue , 2015, Pages 321-334

  Kurakula, Mallesh ^a   El Helw, A M ^a   Sobahi, Tariq R ^a   Abdelaal, Magdy Y ^a  

^a KING ABDULAZIZ UNIVERSITY   (Saudi Arabia)

Author keywords

Anti hyperlipidemia; Atorvastatin; Cationic charge; Chitosan; In vivo efficacy; Nanocrystals; Stability

Indexed keywords

ATORVASTATIN; CHITOSAN; LABRASOL; NANOCRYSTAL; ANTILIPEMIC AGENT; CATION; LIPID; NANOPARTICLE;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CHEMICAL INTERACTION; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG EFFICACY; DRUG FORMULATION; DRUG SOLUBILITY; DRUG STABILITY; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HYPERLIPIDEMIA; IN VITRO STUDY; IN VIVO STUDY; INFRARED SPECTROSCOPY; MALE; MOLECULAR WEIGHT; MORPHOLOGY; NONHUMAN; PARTICLE SIZE; PH; PHYSICAL CHEMISTRY; RAT; SCANNING ELECTRON MICROSCOPY; X RAY POWDER DIFFRACTION; ZETA POTENTIAL; ANIMAL; BLOOD; CHEMISTRY; WISTAR RAT;

ANIMALS; ATORVASTATIN CALCIUM; CATIONS; CHITOSAN; DRUG STABILITY; HYPOLIPIDEMIC AGENTS; LIPIDS; MALE; NANOPARTICLES; PARTICLE SIZE; RATS, WISTAR;

EID: 84920911899     PISSN: 11769114     EISSN: 11782013     Source Type: Journal    
DOI: 10.2147/IJN.S77731     Document Type: Article

References (36)

1. Kidane A, Bhatt PP. Recent advances in small molecule drug delivery. Curr Opin Chem Biol. 2005;9(4):347–351.
2. Wang B, Siahaan TJ, Soltero RA. Drug delivery: principles and applica­tions. New Jersey: John Wiley and Sons; 2005.
3. Williams HD, Trevaskis NL, Charman SA, et al. Strategies to Address Low Drug Solubility in Discovery and Development. Pharmacol Rev. 2013;65(1):1315–1499.
4. Liversidge GG, Conzentino P. Drug particle size reduction for decreas­ing gastric irritancy and enhancing absorption of naproxen in rats. Int J Pharm. 1995;125(2):309–313.
5. Kasim NA, Whitehouse M, Ramachandran C, et al. Molecular Properties of WHO Essential Drugs and Provisional Biopharmaceutical Classification. Mol Pharm. 2004;1(1):85–96.
6. Cilla DD Jr, Whitfield LR, Gibson DM, Sedman AJ, Posvar EL. Multiple-dose pharmacokinetics, pharmacodynamics, and safety of atorvastatin, an inhibitor of HMG-CoA reductase, in healthy subjects. Clin Pharmacol Ther. 1996;60(6):687–695.
7. Law MR, Wald NJ, Rudnicka AR. Quantifying effect of statins on low density lipoprotein cholesterol, ischaemic heart disease, and stroke: systematic review and meta-analysis. BMJ. 2003;326(7404):1423.
8. Kim JS, Kim MS, Park HJ, Jin SJ, Lee S, Hwang SJ. Physicochemi­cal properties and oral bioavailability of amorphous atorvastatin hemi-calcium using spray-drying and SAS process. Int J Pharm. 2008;359(1–2):211–219.
9. Lau HH, Okochi H, Huang Y, Benet LZ. Pharmacokinetics of atorvas­tatin and its hydroxymetabolites in rats and the effects of concomitant rifampicin single doses: relevance of first-pass effect from hepatic uptake transporters, and intestinal and hepatic metabolism. Drug Metab Dispos. 2006;34(7):1175–1181.
10. Lennernas H. Human jejunal effective permeability and its correla­tion with preclinical drug absorption models. J Pharm Pharmacol. 1997;49(7):627–638.
11. Lennernas H. Clinical pharmacokinetics of atorvastatin. Clin Pharma­cokinet. 2003;42(13):1141–1160.
12. Kadu PJ, Kushare SS, Thacker DD, Gattani SG. Enhancement of oral bioavailability of atorvastatin calcium by self-emulsifying drug delivery systems (SEDDS). Pharm Dev Technol. 2011;16(1):65–74.
13. Shen H, Zhong M. Preparation and evaluation of self-micro emulsifying drug delivery systems (SMEDDS) containing atorvastatin. J Pharm and Pharmcol. 2006;58(9):1183–1191.
14. Miryala V, Kurakula M. Self-nano emulsifying drug delivery systems (SNEDDS) for oral delivery of atorvastatin -formulation and bioavailability studies. J Drug Deliv Therap. 2013;3:131–142.
15. Kim M, Jin S, Kim J, et al. Preparation, characterization and in vivo evaluation of amorphous atorvastatin calcium nanoparticles using supercritical antisolvent (SAS) process. Eur J Pharm Biopharm. 2008;69(2):454–465.
16. Zhang HX, Wang JX, Zhang ZB, Le Y, Shen ZG, Chen JF. Microniza­tion of atorvastatin calcium by antisolvent precipitation process. Int J Pharm. 2009;374(1–2):106–113.
17. Junghanns JU, Muller RH. Nanocrystal technology drug delivery and clinical applications. Int J Nanomedicine. 2008;3(3):295–310.
18. Moschwitzer JP. Drug nanocrystals in the commercial pharmaceutical development process. Int J Pharm. 2013;453(1):142–156.
19. Keck CM, Muller RH. Drug nanocrystals of poorly soluble drugs produced by high pressure homogenisation. Eur J Pharm Biopharm. 2006;62(1):3–16.
20. Crisp MT, Tucker CJ, Rogers TL, William RO 3rd, Johnston KP. Turbidimetric measurement and prediction of dissolution rate of poor soluble drug nanocrystals. J Control Release. 2007;117(3):351–359.
21. Jinno J, Kamada N, Miyaki M, et al. Effect of particle size reduction on dissolution and oral absorption of poor soluble drugs. J Control Release. 2006;111(1–2):56–64.
22. Delongeas JL, Vermeil de Conchard G, Beamonte A, et al. Assessment Labrasol/Labrafil/Transcutol (4/4/2, v/v/v) as a non-clinical vehicle for poorly water-soluble compounds after 4-week oral toxicity study in Wistar rats. Regul Toxicol Pharm. 2010;57(2–3):284–290.
23. Sun W, Tian W, Zhang Y, He J, Mao S, Fang L. Effect of novel stabilizers cationic polymers on the particle size and physical stability of poorly soluble drug nanocrystals. Nanomedicine. 2012;8(4):460–467.
24. Muzzarelli RA. Human enzymatic activities related to therapeutic administration of chitin derivatives. Cell Mol Life Sci. 1997;53(2):131–140.
25. Hirano S, Seino H, Akiyama Y, Nonaka I. Chitosan: a biocompatible material for oral and intravenous administration, in Oral and Intravenous Administrations. Progress in Biomedical Polymers. 1990;283–289.
26. Mao S, Sun W, Kissel T. Chitosan-based formulations for delivery of DNA and siRNA. Adv Drug Deliv Rev. 2010;62(1):12–27.
27. Mao S, Shuai X, Unger F, Simon M, Bi D, Kissel T. The depolymerisa­tion of chitosan: effects on physiochemical and biological properties. Int J Pharm. 2004;281(1–2):45–54.
28. Lee E, Kim H, Lee IH, Jon S. In vivo antitumor effects of chitosan-conjugated docetaxel after oral administration. J Control Release. 2009;140(2):79–85.
29. Lee E, Lee J, Lee IH, et al. Conjugated chitosan as a novel platform for oral delivery of paclitaxel. J Med Chem. 2008;51(20):6442–6449.
30. Dos Santos S, Medronho B, Santos TD, Antunes FE. Amphiphilic Molecules in Drug Delivery Systems. Advan Pred Preven Person Med. 2013;435–485.
31. Lu Y, Wang ZH, Li T, Nally HM, Park K, Sturek M. Development and evaluation of transferrin-stabilized paclitaxel nanocrystal formulation. J Control Release. 2014;176:76–85.
32. Fu Q, Sun J, Ai X, et al. Nimodipine nanocrystals for oral bioavailability improvement: Role of mesenteric lymph transport in the oral absorption. Int J Pharm. 2013;448(1):290–297.
33. Chaudhary HR, Brocks DR. The single dose poloxamer 407 model of hyperlipidemia; systemic effects on lipids assessed using pharma­cokinetic methods, and its effects on adipokines. J Pharm Pharm Sci. 2013;16(1):65–73.
34. International Conference on Harmonization [homepage on the Inter­net]. ICH Harmonized Tripartite guideline. Validation of Analytical Procedures: Text and Methodology Q2 (R1). Current Step 4 version. Parent Guideline dated 27 October 1994. (Complementary Guideline on Methodology dated 6 November 1996; incorporated in November 2005). Available from: http://www.ich.org/fileadmin/Public_Web_Site/ICH_Products/Guidelines/Quality/Q2_R1/Step4/Q2_R1__Guideline.pdf. Accessed December 11, 2014.
35. Kurakula M, Sobahi TR, El-Helw AM, Abdelaal MY. Development and Validation of a RP-HPLC Method for Assay of Atorvastatin and its Application in Dissolution Studies on Thermosensitive Hydrogel-Based Nanocrystals. Trop J Pharm Res. 2014;13(10):1681–1687.
36. International Conference on Harmonization [homepage on the Internet]. ICH Harmonized Tripartite guideline. Q1A (R2) Stability Testing of New Drug Substances and Products. Step 4; 2003. Available from: http://www.ich.org/fileadmin/Public_Web_Site/ICH_Products/Guidelines/Quality/Q1A_R2/Step4/Q1A_R2__Guideline.pdf. Accessed December 11, 2014.