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Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery

  • Review Article
  • Theme: Advanced Technologies for Oral Controlled Release
  • Published:
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Abstract

Lipid nanoparticles based on solid matrix have emerged as potential drug carriers to improve gastrointestinal (GI) absorption and oral bioavailability of several drugs, especially lipophilic compounds. These formulations may also be used for sustained drug release. Solid lipid nanoparticle (SLN) and the newer generation lipid nanoparticle, nanostructured lipid carrier (NLC), have been studied for their capability as oral drug carriers. Biodegradable, biocompatible, and physiological lipids are generally used to prepare these nanoparticles. Hence, toxicity problems related with the polymeric nanoparticles can be minimized. Furthermore, stability of the formulations might increase than other liquid nano-carriers due to the solid matrix of these lipid nanoparticles. These nanoparticles can be produced by different formulation techniques. Scaling up of the production process from lab scale to industrial scale can be easily achieved. Reasonably high drug encapsulation efficiency of the nanoparticles was documented. Oral absorption and bioavailability of several drugs were improved after oral administration of the drug-loaded SLNs or NLCs. In this review, pros and cons, different formulation and characterization techniques, drug incorporation models, GI absorption and oral bioavailability enhancement mechanisms, stability and storage condition of the formulations, and recent advances in oral delivery of the lipid nanoparticles based on solid matrix will be discussed.

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References

  1. Mehnert W, Mader K. Solid lipid nanoparticles: production, characterization and applications. Adv Drug Deliv Rev. 2001;47(2–3):165–96.

    PubMed  CAS  Google Scholar 

  2. Muller RH, Mader K, Gohla S. Solid lipid nanoparticles (SLN) for controlled drug delivery—a review of the state of the art. Eur J Pharm Biopharm. 2000;50(1):161–77.

    PubMed  CAS  Google Scholar 

  3. Radtke M, Souto EB, Müller RH. Nanostructured Lipid Carriers: a novel generation of solid lipid drug carriers. Pharm Technol Eur. 2005;17(4):45–50.

    CAS  Google Scholar 

  4. Pouton CW. Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system. Eur J Pharm Sci. 2006;29(3–4 SPEC. ISS):278–87.

    PubMed  CAS  Google Scholar 

  5. Muller RH, Maassen S, Weyhers H, Mehnert W. Phagocytic uptake and cytotoxicity of solid lipid nanoparticles (SLN) sterically stabilized with poloxamine 908 and poloxamer 407. J Drug Target. 1996;4(3):161–70.

    PubMed  CAS  Google Scholar 

  6. Ravi Kumar MN. Nano and microparticles as controlled drug delivery devices. J Pharm Pharm Sci. 2000;3(2):234–58.

    PubMed  CAS  Google Scholar 

  7. Shidhaye SS, Vaidya R, Sutar S, Patwardhan A, Kadam VJ. Solid lipid nanoparticles and nanostructured lipid carriers—innovative generations of solid lipid carriers. Curr Drug Deliv. 2008;5(4):324–31.

    PubMed  CAS  Google Scholar 

  8. Chen DB, Yang TZ, Lu WL, Zhang Q. In vitro and in vivo study of two types of long-circulating solid lipid nanoparticles containing paclitaxel. Chem Pharm Bull. 2001;49(11):1444–7.

    PubMed  CAS  Google Scholar 

  9. Fundaro A, Cavalli R, Bargoni A, Vighetto D, Zara GP, Gasco MR. Non-stealth and stealth solid lipid nanoparticles (SLN) carrying doxorubicin: pharmacokinetics and tissue distribution after i.v. administration to rats. Pharmacol Res. 2000;42(4):337–43.

    PubMed  CAS  Google Scholar 

  10. Freitas C, Muller RH. Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLN®) dispersions. Int J Pharm. 1998;168(2):221–9.

    CAS  Google Scholar 

  11. Freitas C, Muller RH. Correlation between long-term stability of solid lipid nanoparticles (SLN(TM)) and crystallinity of the lipid phase. Eur J Pharm Biopharm. 1999;47(2):125–32.

    PubMed  CAS  Google Scholar 

  12. Freitas C, Muller RH. Stability determination of solid lipid nanoparticles (SLN®) in aqueous dispersion after addition of electrolyte. J Microencapsul. 1999;16(1):59–71.

    PubMed  CAS  Google Scholar 

  13. Dingler A, Gohla S. Production of solid lipid nanoparticles (SLN): scaling up feasibilities. J Microencapsul. 2002;19(1):11–6.

    PubMed  CAS  Google Scholar 

  14. Gohla SH, Dingler A. Scaling up feasibility of the production of solid lipid nanoparticles (SLN). Pharmazie. 2001;56(1):61–3.

    PubMed  CAS  Google Scholar 

  15. Manjunath K, Ready JS, Venkateswarlu V. Solid lipid nanoparticles as drug delivery systems. Meth Find Exp Clin Pharmacol. 2005;27(2):127–44.

    CAS  Google Scholar 

  16. Charman WN. Lipids, lipophilic drugs, and oral drug delivery—some emerging concepts. J Pharm Sci. 2000;89(8):967–78.

    PubMed  CAS  Google Scholar 

  17. Charman WN, Porter CJH, Mithani S, Dressman JB. Physicochemical and physiological mechanisms for the effects of food on drug absorption: the role of lipids and pH. J Pharm Sci. 1997;86(3):269–82.

    PubMed  CAS  Google Scholar 

  18. Charman WN, Porter CJH. Lipophilic prodrugs designed for intestinal lymphatic transport. Adv Drug Deliv Rev. 1996;19(2):149–69.

    CAS  Google Scholar 

  19. Holm R, Porter CJH, Mullertz A, Kristensen HG, Charman WN. Structured triglyceride vehicles for oral delivery of halofantrine: examination of intestinal lymphatic transport and bioavailability in conscious rats. Pharm Res. 2002;19(9):1354–61.

    PubMed  CAS  Google Scholar 

  20. Porter CJH, Charman WN. Intestinal lymphatic drug transport: an update. Adv Drug Deliv Rev. 2001;50(1–2):61–80.

    PubMed  CAS  Google Scholar 

  21. Kaur IP, Bhandari R, Bhandari S, Kakkar V. Potential of solid lipid nanoparticles in brain targeting. J Control Release. 2008;127(2):97–109.

    PubMed  CAS  Google Scholar 

  22. Chen Y, Dalwadi G, Benson HA. Drug delivery across the blood–brain barrier. Curr Drug Deliv. 2004;1(4):361–76.

    PubMed  CAS  Google Scholar 

  23. Souto EB, Doktorovova S, Gonzalez-Mira E, Egea MA, Garcia ML. Feasibility of lipid nanoparticles for ocular delivery of anti-inflammatory drugs. Curr Eye Res. 2010;35(7):537–52.

    PubMed  CAS  Google Scholar 

  24. Pardeike J, Hommoss A, Müller RH. Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products. Int J Pharm. 2009;366(1–2):170–84.

    PubMed  CAS  Google Scholar 

  25. Wissing SA, Kayser O, Muller RH. Solid lipid nanoparticles for parenteral drug delivery. Adv Drug Deliv Rev. 2004;56(9):1257–72.

    PubMed  CAS  Google Scholar 

  26. Garcia-Fuentes M, Prego C, Torres D, Alonso MJ. A comparative study of the potential of solid triglyceride nanostructures coated with chitosan or poly(ethylene glycol) as carriers for oral calcitonin delivery. Eur J Pharm Sci. 2005;25(1):133–43.

    PubMed  CAS  Google Scholar 

  27. Manjunath K, Venkateswarlu V. Pharmacokinetics, tissue distribution and bioavailability of clozapine solid lipid nanoparticles after intravenous and intraduodenal administration. J Control Release. 2005;107(2):215–28.

    PubMed  CAS  Google Scholar 

  28. Tsai MJ, Huang YB, Wu PC, Fu YS, Kao YR, Fang JY, et al. Oral apomorphine delivery from solid lipid nanoparticleswith different monostearate emulsifiers: Pharmacokinetic and behavioral evaluations. J Pharm Sci. 2010 (in press).

  29. Varshosaz J, Minayian M, Moazen E. Enhancement of oral bioavailability of pentoxifylline by solid lipid nanoparticles. J Liposome Res. 2010;20(2):115–23.

    PubMed  CAS  Google Scholar 

  30. Varshosaz J, Tabbakhian M, Mohammadi MY. Formulation and optimization of solid lipid nanoparticles of buspirone HCl for enhancement of its oral bioavailability. J Liposome Res. 2010;20(4):286–96.

    PubMed  CAS  Google Scholar 

  31. Kumar VV, Chandrasekar D, Ramakrishna S, Kishan V, Rao YM, Diwan PV. Development and evaluation of nitrendipine loaded solid lipid nanoparticles: influence of wax and glyceride lipids on plasma pharmacokinetics. Int J Pharm. 2007;335(1–2):167–75.

    PubMed  CAS  Google Scholar 

  32. Sarmento B, Martins S, Ferreira D, Souto EB. Oral insulin delivery by means of solid lipid nanoparticles. Int J Nanomedicine. 2007;2(4):743–9.

    PubMed  CAS  Google Scholar 

  33. Kakkar V, Singh S, Singla D, Kaur IP. Exploring solid lipid nanoparticles to enhance the oral bioavailability of curcumin. Mol Nutr Food Res. 2010 (in press).

  34. Yang R, Gao R, Li F, He H, Tang X. The influence of lipid characteristics on the formation, in vitro release, and in vivo absorption of protein-loaded SLN prepared by the double emulsion process. Drug Dev Ind Pharm. 2010 (in press).

  35. Hu L, Xing Q, Meng J, Shang C. Preparation and enhanced oral bioavailability of cryptotanshinone-loaded solid lipid nanoparticles. AAPS PharmSciTech. 2010;11(2):582–7.

    PubMed  Google Scholar 

  36. Hu L, Jia H, Luo Z, Liu C, Xing Q. Improvement of digoxin oral absorption in rabbits by incorporation into solid lipid nanoparticles. Pharmazie. 2010;65(2):110–3.

    PubMed  CAS  Google Scholar 

  37. Hu L, Tang X, Cui F. Solid lipid nanoparticles (SLNs) to improve oral bioavailability of poorly soluble drugs. J Pharm Pharmacol. 2004;56(12):1527–35.

    PubMed  CAS  Google Scholar 

  38. Paliwal R, Rai S, Vaidya B, Khatri K, Goyal AK, Mishra N, et al. Effect of lipid core material on characteristics of solid lipid nanoparticles designed for oral lymphatic delivery. Nanomedicine NBM. 2009;5(2):184–91.

    CAS  Google Scholar 

  39. Luo Y, Chen D, Ren L, Zhao X, Qin J. Solid lipid nanoparticles for enhancing vinpocetine’s oral bioavailability. J Control Release. 2006;114(1):53–9.

    PubMed  CAS  Google Scholar 

  40. Chen CC, Tsai TH, Huang ZR, Fang JY. Effects of lipophilic emulsifiers on the oral administration of lovastatin from nanostructured lipid carriers: physicochemical characterization and pharmacokinetics. Eur J Pharm Biopharm. 2010;74(3):474–82.

    PubMed  CAS  Google Scholar 

  41. Martins S, Silva AC, Ferreira DC, Souto EB. Improving oral absorption of samon calcitonin by trimyristin lipid nanoparticles. J Biomed Nanotechnol. 2009;5(1):76–83.

    PubMed  CAS  Google Scholar 

  42. Muller RH, Runge SA, Ravelli V, Thunemann AF, Mehnert W, Souto EB. Cyclosporine-loaded solid lipid nanoparticles (SLN®): drug-lipid physicochemical interactions and characterization of drug incorporation. Eur J Pharm Biopharm. 2008;68(3):535–44.

    PubMed  CAS  Google Scholar 

  43. Muller RH, Runge S, Ravelli V, Mehnert W, Thunemann AF, Souto EB. Oral bioavailability of cyclosporine: solid lipid nanoparticles (SLN®) versus drug nanocrystals. Int J Pharm. 2006;317(1):82–9.

    PubMed  CAS  Google Scholar 

  44. Saupe A, Gordon KC, Rades T. Structural investigations on nanoemulsions, solid lipid nanoparticles and nanostructured lipid carriers by cryo-field emission scanning electron microscopy and Raman spectroscopy. Int J Pharm. 2006;314(1):56–62.

    PubMed  CAS  Google Scholar 

  45. Müller RH, Radtke M, Wissing SA. Nanostructured lipid matrices for improved microencapsulation of drugs. Int J Pharm. 2002;242(1–2):121–8.

    PubMed  Google Scholar 

  46. Müller RH, Radtke M, Wissing SA. Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv Drug Deliv Rev. 2002;54(Supplement 1):S131–55.

    PubMed  Google Scholar 

  47. Westesen K, Bunjes H, Koch MHJ. Physicochemical characterization of lipid nanoparticles and evaluation of their drug loading capacity and sustained release potential. J Control Release. 1997;48(2–3):223–36.

    CAS  Google Scholar 

  48. Jenning V, Lippacher A, Gohla SH. Medium scale production of solid lipid nanoparticles (SLN) by high pressure homogenization. J Microencapsul. 2002;19(1):1–10.

    PubMed  CAS  Google Scholar 

  49. Cavalli R, Caputo O, Marengo E, Pattarino F, Gasco MR. The effect of the components of microemulsions on both size and crystalline structure of solid lipid nanoparticles (SLN) containing a series of model molecules. Pharmazie. 1998;53(6):392–6.

    CAS  Google Scholar 

  50. Schwarz C. Solid lipid nanoparticles (SLN) for controlled drug delivery. I. Production, characterization and sterilization. J Control Release. 1994;30(1):83–96.

    CAS  Google Scholar 

  51. Muchow M, Maincent P, Muller RH. Lipid nanoparticles with a solid matrix (SLN®, NLC®, LDC®) for oral drug delivery. Drug Dev Ind Pharm. 2008;34(12):1394–405.

    PubMed  CAS  Google Scholar 

  52. Müller RH, Lucks JS, inventors; Arzneistoffträger aus festen Lipidteilchen, Feste Lipidnanosphären (SLN)/medication vehicles made of solid lipid particles (solid lipid nanospheres–SLN) patent EP 0605497 B1. 1996.

  53. Gasco MR, inventor Gasco, M. R., assignee. Method for producing solid lipid microspheres having a narrow size distribution patent US5250236. 1993.

  54. Cortesi R, Esposito E, Luca G, Nastruzzi C. Production of lipospheres as carriers for bioactive compounds. Biomaterials. 2002;23(11):2283–94.

    PubMed  CAS  Google Scholar 

  55. Igartua M, Saulnier P, Heurtault B, Pech B, Proust JE, Pedraz JL, et al. Development and characterization of solid lipid nanoparticles loaded with magnetite. Int J Pharm. 2002;233(1–2):149–57.

    PubMed  CAS  Google Scholar 

  56. Bondi ML, Azzolina A, Craparo EF, Lampiasi N, Capuano G, Giammona G, et al. Novel cationic solid-lipid nanoparticles as non-viral vectors for gene delivery. J Drug Target. 2007;15(4):295–301.

    PubMed  CAS  Google Scholar 

  57. Sjostrom B, Kaplun A, Talmon Y, Cabane B. Structures of nanoparticles prepared from oil-in-water emulsions. Pharm Res. 1995;12(1):39–48.

    PubMed  CAS  Google Scholar 

  58. Shahgaldian P, Da Silva E, Coleman AW, Rather B, Zaworotko MJ. Para-acyl-calix-arene based solid lipid nanoparticles (SLNs): a detailed study of preparation and stability parameters. Int J Pharm. 2003;253(1–2):23–38.

    PubMed  CAS  Google Scholar 

  59. Trotta M, Debernardi F, Caputo O. Preparation of solid lipid nanoparticles by a solvent emulsification–diffusion technique. Int J Pharm. 2003;257(1–2):153–60.

    PubMed  CAS  Google Scholar 

  60. Hu FQ, Yuan H, Zhang HH, Fang M. Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization. Int J Pharm. 2002;239(1–2):121–8.

    PubMed  CAS  Google Scholar 

  61. Schubert MA, Muller-Goymann CC. Solvent injection as a new approach for manufacturing lipid nanoparticles—evaluation of the method and process parameters. Eur J Pharm Biopharm. 2003;55(1):125–31.

    PubMed  CAS  Google Scholar 

  62. Charman WN, Stella VJ, editors. Lymphatic transport of drugs. Boca Raton: CRC Press; 1992.

    Google Scholar 

  63. Radomska-Soukharev A. Stability of lipid excipients in solid lipid nanoparticles. Adv Drug Deliv Rev. 2007;59(6):411–8.

    PubMed  CAS  Google Scholar 

  64. Xie S, Pan B, Wang M, Zhu L, Wang F, Dong Z, et al. Formulation, characterization and pharmacokinetics of praziquantel-loaded hydrogenated castor oil solid lipid nanoparticles. Nanomedicine Lond. 2010;5(5):693–701.

    PubMed  CAS  Google Scholar 

  65. Liu DH, Liu CX, Zou WW, Zhang N. Enhanced gastrointestinal absorption of N-3-O-toluyl-fluorouracil by cationic solid lipid nanoparticles. J Nanopart Res. 2010;12(3):975–84.

    CAS  Google Scholar 

  66. Zhang J, Fan Y, Smith E. Experimental design for the optimization of lipid nanoparticles. J Pharm Sci. 2009;98(5):1813–9.

    PubMed  CAS  Google Scholar 

  67. Anton N, Benoit J-P, Saulnier P. Design and production of nanoparticles formulated from nano-emulsion templates—a review. J Control Release. 2008;128(3):185–99.

    PubMed  CAS  Google Scholar 

  68. Sanjula B, Shah FM, Javed A, Alka A. Effect of poloxamer 188 on lymphatic uptake of carvedilol-loaded solid lipid nanoparticles for bioavailability enhancement. J Drug Target. 2009;17(3):249–56.

    PubMed  CAS  Google Scholar 

  69. Freitas C, Müller RH. Effect of light and temperature on zeta potential and physical stability in solid lipid nanoparticle (SLN(TM)) dispersions. Int J Pharm. 1998;168(2):221–9.

    CAS  Google Scholar 

  70. Mukherjee B, Santra K, Pattnaik G, Ghosh S. Preparation, characterization and in vitro evaluation of sustained release protein-loaded nanoparticles based on biodegradable polymers. Int J Nanomedicine. 2008;3(4):487–96.

    PubMed  CAS  Google Scholar 

  71. Sahana B, Santra K, Basu S, Mukherjee B. Development of biodegradable polymer-based tamoxifen citrate-loaded nanoparticles and effect of some manufacturing process parameters on them: a physicochemical and in vitro evaluation. Int J Nanomedicine. 2010;5:621–30.

    PubMed  CAS  Google Scholar 

  72. Zur Muhlen A, Zur Muhlen E, Niehus H, Mehnert W. Atomic force microscopy studies of solid lipid nanoparticles. Pharm Res. 1996;13(9):1411–6.

    PubMed  Google Scholar 

  73. Souto EB, Mehnert W, Muller RH. Polymorphic behaviour of Compritol888 ATO as bulk lipid and as SLN and NLC. J Microencapsul. 2006;23(4):417–33.

    PubMed  CAS  Google Scholar 

  74. Estella-Hermoso de Mendoza A, Campanero MA, Mollinedo F, Blanco-Prieto MJ. Lipid nanomedicines for anticancer drug therapy. J Biomed Nanotechnol. 2009;5(4):323–43.

    PubMed  CAS  Google Scholar 

  75. Bunjes H, Steiniger F, Richter W. Visualizing the structure of triglyceride nanoparticles in different crystal modifications. Langmuir. 2007;23(7):4005–11.

    PubMed  CAS  Google Scholar 

  76. Estella-Hermoso de Mendoza A, Rayo M, Mollinedo F, Blanco-Prieto MJ. Lipid nanoparticles for alkyl lysophospholipid edelfosine encapsulation: development and in vitro characterization. Eur J Pharm Biopharm. 2008;68(2):207–13.

    PubMed  CAS  Google Scholar 

  77. Jenning V, Mader K, Gohla SH. Solid lipid nanoparticles (SLN) based on binary mixtures of liquid and solid lipids: a (1)H-NMR study. Int J Pharm. 2000;205(1–2):15–21.

    PubMed  CAS  Google Scholar 

  78. Küchler S, Herrmann W, Panek-Minkin G, Blaschke T, Zoschke C, Kramer KD, et al. SLN for topical application in skin diseases—characterization of drug–carrier and carrier–target interactions. Int J Pharm. 2010;390(2):225–33.

    PubMed  Google Scholar 

  79. Zimmermann E, Souto EB, Muller RH. Physicochemical investigations on the structure of drug-free and drug-loaded solid lipid nanoparticles (SLN) by means of DSC and 1H NMR. Pharmazie. 2005;60(7):508–13.

    PubMed  CAS  Google Scholar 

  80. Braem C, Blaschke T, Panek-Minkin G, Herrmann W, Schlupp P, Paepenmüller T, et al. Interaction of drug molecules with carrier systems as studied by parelectric spectroscopy and electron spin resonance. J Control Release. 2007;119(1):128–35.

    PubMed  CAS  Google Scholar 

  81. Lukowski G, Hoell A, Dingler A, Kranold R, Pflegel P. Fractal surface of solid lipid nanoparticles. Proc Control Release Society. 1997;24:631–2.

    Google Scholar 

  82. Muller RH, Mehnert W, Lucks JS, Schwarz C, Zur Muhlen A, Weyhers H, et al. Solid lipid nanoparticles (SLN)—an alternative colloidal carrier system for controlled drug delivery. Eur J Pharm Biopharm. 1995;41(1):62–9.

    CAS  Google Scholar 

  83. Zur Muhlen A, Mehnert W. Drug release and release mechanism of prednisolone loaded solid lipid nanoparticles. Pharmazie. 1998;53(8):552–5.

    Google Scholar 

  84. Chakraborty S, Shukla D, Mishra B, Singh S. Lipid—an emerging platform for oral delivery of drugs with poor bioavailability. Eur J Pharm Biopharm. 2009;73(1):1–15.

    PubMed  CAS  Google Scholar 

  85. Crounse RG. Human pharmacology of griseofulvin: the effect of fat intake on gastrointestinal absorption. J Invest Dermatol. 1961;37:529–33.

    PubMed  CAS  Google Scholar 

  86. Horter D, Dressman JB. Influence of physicochemical properties on dissolution of drugs in the gastrointestinal tract. Adv Drug Deliv Rev. 2001;46(1–3):75–87.

    PubMed  CAS  Google Scholar 

  87. Wagner D, Spahn-Langguth H, Hanafy A, Koggel A, Langguth P. Intestinal drug efflux: formulation and food effects. Adv Drug Deliv Rev. 2001;50 Suppl 1:S13–31.

    PubMed  CAS  Google Scholar 

  88. Touitou E, Barry BW, editors. Enhancement in drug delivery. Florida: CRC Press; 2006.

    Google Scholar 

  89. Liversidge GG, Cundy KC. Particle size reduction for improvement of oral bioavailability of hydrophobic drugs: I. Absolute oral bioavailability of nanocrystalline danazol in beagle dogs. Int J Pharm. 1995;125(1):91–7.

    CAS  Google Scholar 

  90. Charman SA, Charman WN, Rogge MC, Wilson TD, Dutko FJ, Pouton CW. Self-emulsifying drug delivery systems: formulation and biopharmaceutic evaluation of an investigational lipophilic compound. Pharm Res. 1992;9(1):87–93.

    PubMed  CAS  Google Scholar 

  91. Li C, Fleisher D, Li L, Schwier JR, Sweetana SA, Vasudevan V, et al. Regional-dependent intestinal absorption and meal composition effects on systemic availability of LY303366, a lipopeptide antifungal agent, in dogs. J Pharm Sci. 2001;90(1):47–57.

    PubMed  CAS  Google Scholar 

  92. Martinez M, Amidon G, Clarke L, Jones WW, Mitra A, Riviere J. Applying the biopharmaceutics classification system to veterinary pharmaceutical products. Part II. Physiological considerations. Adv Drug Deliv Rev. 2002;54(6):825–50.

    PubMed  CAS  Google Scholar 

  93. Trevaskis NL, Charman WN, Porter CJ. Lipid-based delivery systems and intestinal lymphatic drug transport: a mechanistic update. Adv Drug Deliv Rev. 2008;60(6):702–16.

    PubMed  CAS  Google Scholar 

  94. Khoo SM, Shackleford DM, Porter CJH, Edwards GA, Charman WN. Intestinal lymphatic transport of halofantrine occurs after oral administration of a unit–dose lipid-based formulation to fasted dogs. Pharm Res. 2003;20(9):1460–5.

    PubMed  CAS  Google Scholar 

  95. Wang D, Wang X, Li X, Ye L. Preparation and characterization of solid lipid nanoparticles loaded with α-asarone. PDA J Pharm Sci Technol. 2008;62(1):56–65.

    PubMed  CAS  Google Scholar 

  96. Yang S, Zhu J, Lu Y, Liang B, Yang C. Body distribution of camptothecin solid lipid nanoparticles after oral administration. Pharm Res. 1999;16(5):751–7.

    PubMed  CAS  Google Scholar 

  97. Bekerman T, Golenser J, Domb A. Cyclosporin nanoparticulate lipospheres for oral administration. J Pharm Sci. 2004;93(5):1264–70.

    PubMed  CAS  Google Scholar 

  98. Hanafy A, Spahn-Langguth H, Vergnault G, Grenier P, Tubic Grozdanis M, Lenhardt T, et al. Pharmacokinetic evaluation of oral fenofibrate nanosuspensions and SLN in comparison to conventional suspensions of micronized drug. Adv Drug Deliv Rev. 2007;59(6):419–26.

    PubMed  CAS  Google Scholar 

  99. Zhang N, Ping Q, Huang G, Xu W, Cheng Y, Han X. Lectin-modified solid lipid nanoparticles as carriers for oral administration of insulin. Int J Pharm. 2006;327(1–2):153–9.

    PubMed  CAS  Google Scholar 

  100. Zhang Z, Lv H, Zhou J. Novel solid lipid nanoparticles as carriers for oral administration of insulin. Pharmazie. 2009;64(9):574–8.

    PubMed  CAS  Google Scholar 

  101. Zhang N, Ring Q, Huang G, Han X, Cheng Y, Xu W. Transport characteristics of wheat germ agglutinin-modified insulin-liposomes and solid lipid nanoparticles in a perfused rat intestinal model. J Nanosci Nanotechnol. 2006;6(9–10):2959–66.

    PubMed  CAS  Google Scholar 

  102. Priano L, Esposti D, Esposti R, Castagna G, De Medici C, Fraschini F, et al. Solid lipid nanoparticles incorporating melatonin as new model for sustained oral and transdermal delivery systems. J Nanosci Nanotechnol. 2007;7(10):3596–601.

    PubMed  CAS  Google Scholar 

  103. Liu C, Liu D, Bai F, Zhang J, Zhang N. In vitro and in vivo studies of lipid-based nanocarriers for oral N3-o-toluyl-fluorouracil delivery. Drug Deliv. 2010;17(5):352–63.

    PubMed  CAS  Google Scholar 

  104. Yuan H, Chen J, Du YZ, Hu FQ, Zeng S, Zhao HL. Studies on oral absorption of stearic acid SLN by a novel fluorometric method. Colloids Surf B. 2007;58(2):157–64.

    CAS  Google Scholar 

  105. Yang L, Geng Y, Li H, Zhang Y, You J, Chang Y. Enhancement the oral bioavailability of praziquantel by incorporation into solid lipid nanoparticles. Pharmazie. 2009;64(2):86–9.

    PubMed  CAS  Google Scholar 

  106. Li H, Zhao X, Ma Y, Zhai G, Li L, Lou H. Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles. J Control Release. 2009;133(3):238–44.

    PubMed  CAS  Google Scholar 

  107. Pandey R, Sharma S, Khuller GK. Oral solid lipid nanoparticle-based antitubercular chemotherapy. Tuberculosis. 2005;85(5–6):415–20.

    PubMed  CAS  Google Scholar 

  108. Langguth P, Hanafy A, Frenzel D, Grenier P, Nhamias A, Ohlig T, et al. Nanosuspension formulations for low-soluble drugs: pharmacokinetic evaluation using spironolactone as model compound. Drug Dev Ind Pharm. 2005;31(3):319–29.

    PubMed  CAS  Google Scholar 

  109. Zhuang CY, Li N, Wang M, Zhang XN, Pan WS, Peng JJ, et al. Preparation and characterization of vinpocetine-loaded nanostructured lipid carriers (NLC) for improved oral bioavailability. Int J Pharm. 2010;394(1–2):179–85.

    PubMed  CAS  Google Scholar 

  110. Westesen K. Novel lipid-based colloidal dispersions as potential drug administration systems—expectations and reality. Colloid Polym Sci. 2000;278(7):608–18.

    CAS  Google Scholar 

  111. Freitas C, Müller RH. Correlation between long-term stability of solid lipid nanoparticles (SLN(TM)) and crystallinity of the lipid phase. Eur J Pharm Biopharm. 1999;47(2):125–32.

    PubMed  CAS  Google Scholar 

  112. Freitas C, Mullera RH. Spray-drying of solid lipid nanoparticles (SLN TM). Eur J Pharm Biopharm. 1998;46(2):145–51.

    PubMed  CAS  Google Scholar 

  113. Kramer T, Kremer DM, Pikal MJ, Petre WJ, Shalaev EY, Gatlin LA. A procedure to optimize scale-up for the primary drying phase of lyophilization. J Pharm Sci. 2009;98(1):307–18.

    PubMed  CAS  Google Scholar 

  114. Schwarz C, Mehnert W. Freeze-drying of drug-free and drug-loaded solid lipid nanoparticles (SLN). Int J Pharm. 1997;157(2):171–9.

    PubMed  CAS  Google Scholar 

  115. Heiati H, Tawashi R, Phillips NC. Drug retention and stability of solid lipid nanoparticles containing azidothymidine palmitate after autoclaving, storage and lyophilization. J Microencapsul. 1998;15(2):173–84.

    PubMed  CAS  Google Scholar 

  116. Zimmermann E, Muller RH, Mader K. Influence of different parameters on reconstitution of lyophilized SLN. Int J Pharm. 2000;196(2):211–3.

    PubMed  CAS  Google Scholar 

  117. Lim SJ, Kim CK. Formulation parameters determining the physicochemical characteristics of solid lipid nanoparticles loaded with all-trans retinoic acid. Int J Pharm. 2002;243(1–2):135–46.

    PubMed  CAS  Google Scholar 

  118. del Pozo-Rodríguez A, Solinís MA, Gascón AR, Pedraz JL. Short- and long-term stability study of lyophilized solid lipid nanoparticles for gene therapy. Eur J Pharm Biopharm. 2009;71(2):181–9.

    PubMed  Google Scholar 

  119. Pardeike J, Hommoss A, Muller RH. Lipid nanoparticles (SLN, NLC) in cosmetic and pharmaceutical dermal products. Int J Pharm. 2009;366(1–2):170–84.

    PubMed  CAS  Google Scholar 

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Authors and Affiliations

  1. Institute of Chemical and Engineering Sciences, Agency for Science, Technology and Research, 1 Pesek Road, Jurong Island, Singapore, 627833, Republic of Singapore

    Surajit Das

  2. Department of Pharmacy, National University of Singapore, 18 Science Drive 4, Singapore, 117543, Republic of Singapore

    Anumita Chaudhury

Authors
  1. Surajit Das
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  2. Anumita Chaudhury
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Correspondence to Surajit Das.

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Guest Editors: Michael Repka, Joseph Reo, Linda Felton, and Stephen Howard

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Das, S., Chaudhury, A. Recent Advances in Lipid Nanoparticle Formulations with Solid Matrix for Oral Drug Delivery. AAPS PharmSciTech 12, 62–76 (2011). https://doi.org/10.1208/s12249-010-9563-0

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  • DOI: https://doi.org/10.1208/s12249-010-9563-0

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