A formulation comparison between micro- and nanosuspensions: the importance of particle size for absorption of a model compound, following repeated oral administration to rats during early development

References

• Lipinski CJ. (2001). Avoiding investment in doomed drugs. Is poor solubility an industry wide problem? Curr Drug Discov, 4:17–9.
   Google Scholar
• Lipinski CJ. (2002). Poor aqueous solubility—an industry wide problem in drug discovery. Am Pharm Rev, 5:82–5.
   Google Scholar
• Loftsson T, Brewster ME. (1996). Pharmaceutical applications of cyclodextrins. J Pharm Sci, 85:1017–25.
   PubMed Web of Science ®Google Scholar
• Stella VJ, Rajewski RA. (1997). Cyclodextrins: Their future in drug formulation and delivery. Pharm Res, 14:556–67.
   PubMed Web of Science ®Google Scholar
• Akers MJ. (2002). Excipient-drug interactions in parenteral formulations. J Pharm Sci, 91:2283–300.
   PubMed Web of Science ®Google Scholar
• Rasheed A, Kumar ACK, Sravanthi VVNSS. (2008). Cyclodextrins as drug carrier molecules: A review. Sci Pharm, 76:567–98.
   Google Scholar
• Floyd AG. (1999). Top ten considerations in the development of parenteral emulsions. Pharm Sci Technol Today, 4:134–43.
   PubMedGoogle Scholar
• Lawrence MJ, Rees GD. (2000). Microemulsion-based media as novel drug delivery systems. Adv Drug Deliv Rev, 45:89–121.
   PubMed Web of Science ®Google Scholar
• Nakano M. (2000). Places of emulsions in drug delivery. Adv Drug Deliv Rev, 45:1–4.
   PubMed Web of Science ®Google Scholar
• Serajuddin ATM. (1999). Solid dispersion of poorly water-soluble drugs: Early promises, subsequent problems, and recent breakthroughs. J Pharm Sci, 88:1058–66.
   PubMed Web of Science ®Google Scholar
• Chokshi RJ, Zia H, Sandhu HK, Shah NH, Malick WA. (2007). Improving dissolution rate of poorly water soluble drug by solid dispersion and solid solution—Pros and cons. Drug Deliv, 14:33–45.
   PubMed Web of Science ®Google Scholar
• Serajuddin ATM. (2007). Salt formation to improve drug solubility. Adv Drug Deliv Rev, 59:603–16.
   PubMed Web of Science ®Google Scholar
• Van den Mooter GM, Wuyts N, Blaton R, Busson P, Grobet P. (2001). Physical stabilisation of amorphous ketoconazole in solid dispersions with polyvinylpyrrolidone K25. Eur J Pharm Sci, 12:261–9.
   PubMed Web of Science ®Google Scholar
• Hirasawa N, Ishise S, Miyata H, Danjo K. (2003). An attempt to stabilize nilvadipine solid dispersion by the use of ternary systems. Drug Dev Ind Pharm, 29:997–1004.
   PubMed Web of Science ®Google Scholar
• Weuts I, Kempen D, Verreck G, Decorte A, Heymans K, Peeters J, . (2005). Study of the physicochemical properties and stability of solid dispersions of loperamide and PEG6000 prepared by spray drying. Eur J Pharm Biopharm, 59:119–26.
   PubMed Web of Science ®Google Scholar
• Smikalla MM, Urbanetz NA. (2007). The influence of povidone K17 on the storage stability of solid dispersions of nimodipine and polyethylene glycol. Eur J Pharm Biopharm, 66:106–12.
   PubMed Web of Science ®Google Scholar
• Pudipeddi M, Serajuddin ATM. (2005). Trends in solubility of polymorphs. J Pharm Sci, 94:929–39.
   PubMed Web of Science ®Google Scholar
• Llinas A, Box KJ, Burley JC, Glen RC, Goodman JM. (2007). A new method for the reproducible generation of polymorphs: Two forms of sulindac with very different solubilities. J Appl Crystallogr, 40:379–81.
   Web of Science ®Google Scholar
• Jia L, Wong H, Cerna C, Weitman SD. (2002). Effect of nanonization on absorption of 301029: Ex vivo and in vivo pharmacokinetic correlations determined by liquid chromatography/mass spectrometry. Pharm Res, 19:1091–6.
   PubMed Web of Science ®Google Scholar
• Sigfridsson K, Forssen S, Holländer P, Skantze U, de Verdier J. (2007). A formulation comparison, using a solution and different nanosuspensions of a poorly soluble compound. Eur J Pharm Biopharm, 67:540–7.
   PubMed Web of Science ®Google Scholar
• Gao L, Zhang D, Chen M. (2008). Drug nanocrystals for the formulation of poorly soluble drugs and its application as a potential drug delivery system. J Nanopart Res, 10:845–62.
   Web of Science ®Google Scholar
• Mauludin R, Müller RH, Keck CM. (2009). Kinetic solubility and dissolution velocity of rutin nanocrystals. Eur J Pharm Biopharm, 36:502–10.
   Web of Science ®Google Scholar
• Sigfridsson K, Lundqvist AJ, Strimfors M. (2009). Particle size reduction for improvement of oral absorption of the poorly soluble drug UG558 in rats during early development. Drug Dev Ind Pharm, 35:1479–86.
   PubMed Web of Science ®Google Scholar
• Li X, Gu L, Xu Y, Wang Y. (2009). Preparation of fenofibrate nanosuspension and study of its pharmacokinetic behavior in rats. Drug Dev Ind Pharm, 35:827–33.
   PubMed Web of Science ®Google Scholar
• Kamiya S, Kurita T, Miyagishima A, Arakawa M. (2009). Preparation of griseofulvin nanoparticle suspension by high-pressure homogenization and preservation of the suspension with saccharides and sugar alcohols. Drug Dev Ind Pharm, 35:1022–8.
   PubMed Web of Science ®Google Scholar
• Liversidge GG, Cundy K. (1995). Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs. Int J Pharm, 125:91–7.
   Web of Science ®Google Scholar
• Peters K, Leitzke S, Diederichs JE, Borner K, Hahu H, Müller RH, . (2000). Preparation of a clofazimine nanosuspension for intravenous use and evaluation of its therapeutic efficacy in murine Mycobacterium avium infection. J Antimicrob Chemother, 45:77–83.
   PubMed Web of Science ®Google Scholar
• Pignatello R, Bucolo C, Ferrara P, Maltese A, Puleo A, Puglisi G. (2002). Eudragit RS100 nanosuspensions for the ophthalmic controlled delivery of ibuprofen. Eur J Pharm Sci, 16:53–61.
   PubMed Web of Science ®Google Scholar
• Jacobs C, Müller RH. (2002). Production and characterization of a budesonide nanosuspension for pulmonary administration. Pharm Res, 19:21–4.
   Google Scholar
• Amidon GL, Lennernäs H, Shah VP, Crison JR. (1995). A theoretical basis for a biopharmaceutic drug classification: The correlation of in vitro drug product dissolution and in vivo bioavailability. Pharm Res, 12:413–20.
   PubMed Web of Science ®Google Scholar
• Muller RH, Jacobs C, Kayser O. (2001). Nanosuspensions as particulate drug formulations in therapy. Rationale for development and what we can expect for the future. Adv Drug Deliv Rev, 47:3–19.
   PubMed Web of Science ®Google Scholar
• Kararli TT. (1995). Comparison of the gastrointestinal anatomy, physiology, and biochemistry of humans and commonly used laboratory animals. Biopharm Drug Dispos, 16:351–80.
   PubMed Web of Science ®Google Scholar
• de Zwart LL, Rompelberg CJM, Sips AJAM, Welink J, van Engelen JGM. (1999). Anatomical and physiological differences between various species used in studies on pharmacokinetics and toxicology of xenobiotics. Investigation performed by ‘research for man and environment’ at National Institute of Public Health and Environment, The Netherlands.
   Google Scholar
• Ward FW, Coates ME. (1987). Gastrointestinal pH measurements in rats: Influence of microbial flora, diet, and fasting. Lab Anim, 21:216–22.
   PubMed Web of Science ®Google Scholar
• Noyes AA, Whitney WR. (1897). The rate of solution of solid substances in their own solutions. J Am Chem Soc, 19:930–4.
   Google Scholar
• Sakaguchi E, Itoh H, Uchida S, Horigome T. (1987). Comparison of fibre digestion and digesta retention time between rabbits, guinea pigs, rats and hamsters. Br J Nutr, 58:149–58.
   PubMed Web of Science ®Google Scholar
• DeSesso JM, Jacobson CF. (2001). Anatomical and physiological parameters affecting gastrointestinal absorption in humans and rats. Food Chem Toxicol, 39:209–28.
   PubMed Web of Science ®Google Scholar