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

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

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.

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.

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.

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.

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

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.

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.

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.

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.

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.

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.

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

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

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

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

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.

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

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.

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

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

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

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.

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.

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

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.

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.

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).

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

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.

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.

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.

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).

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).

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.

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.

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.

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.

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.

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.

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.

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.

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.

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.

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

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.

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.

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.

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.

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

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.

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.

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

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

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.

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.

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

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.

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.

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.

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.

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

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

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.

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.

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

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.

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.

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.

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.

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.

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.

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.

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.

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

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.

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.

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.

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.

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.

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

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.

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

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.

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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.

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.

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.

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.

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.

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

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.

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.

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

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.

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.

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.

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.

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.

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.

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

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.

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.

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

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.

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

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.

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

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.

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

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.

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.

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.