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Book cover Lipid Nanoparticles: Production, Characterization and Stability

Part of the book series: SpringerBriefs in Pharmaceutical Science & Drug Development ((BRIEFSPSDD))

Abstract

Highly potent, but poorly water-soluble, drug candidates are common outcomes of lead optimization and other such drug discovery programmes. Poor drug solubility presents several challenges including reduced bioavailability on oral administration, lack of fed-fasted equivalence and abandonment of drug molecules in the early stage of development. Amongst many different strategies for improving drug solubility (e.g. micronization, complexation, prodrug design etc.), development of colloidal carriers has been looked upon as a favourable strategy. A few polymer-based and lipid-based colloidal systems including polymeric nanoparticles, liposomes and emulsions have been well-studied. In this book, the more recent colloidal lipid systems are discussed. Lipid nanoparticles present a viable alternative to other, more traditional, colloidal carriers. These nanoparticles not only have the advantages of most colloidal carriers but also reduce the associated shortcomings. Evolved from parenteral emulsions, lipid nanoparticles are composed of lipid materials that are solid at room and body temperatures, such as triglycerides or fatty acids. Lipid nanoparticle structures can be categorized into four different types: solid lipid nanoparticle (SLN), nanostructured lipid carrier (NLC), lipid drug conjugate (LDC) and polymer-lipid hybrid nanoparticle (PLN). These lipid nanoparticles can encapsulate hydrophilic and lipophilic drugs equally well and may potentially act as the next generation of drug carriers applied in pharmaceuticals. This book focuses on the composition, structure, production, characterization and stability of lipid nanoparticles. Particular emphasis has been given to solid lipid nanoparticles and nanostructured lipid carriers.

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References

  • Attama A, Reichl S, Müller-Goymann C (2008) Diclofenac sodium delivery to the eye: in vitro evaluation of novel solid lipid nanoparticle formulation using human cornea construct. Int J Pharm 355(1–2):307–313

    Article  CAS  PubMed  Google Scholar 

  • Bikiaris D (2011) Solid dispersions, part II: new strategies in manufacturing methods for dissolution rate enhancement of poorly water-soluble drugs. Expert Opin Drug Del. 8(12):1663–1680

    Article  CAS  Google Scholar 

  • Bunjes H, Siekmann B (2005) Manufacture, characterization, and applications of solid lipid nanoparticles as drug delivery systems. Microencapsulation: methods and industrial applications. Drugs and the pharmaceutical sciences. CRC Press, USA p 213–268

    Google Scholar 

  • Cavalli R, Gasco M, Chetoni P, Burgalassi S, Saettone M (2002) Solid lipid nanoparticles (SLN) as ocular delivery system for tobramycin. Int J Pharm 238(1–2):241–245

    Article  CAS  PubMed  Google Scholar 

  • Chattopadhyay P, Shekunov B, Yim D, Cipolla D, Boyd B, Farr S (2007) Production of solid lipid nanoparticle suspensions using supercritical fluid extraction of emulsions (SFEE) for pulmonary delivery using the AERx system. Adv Drug Deliver Rev 59(6):444–453

    Article  CAS  Google Scholar 

  • Das S, Chaudhury A (2011) Recent advances in lipid nanoparticle formulations with solid matrix for oral drug delivery. AAPS PharmSciTech 12(1):62–76

    Article  CAS  PubMed Central  PubMed  Google Scholar 

  • de Mendoza A, Campanero M, Mollinedo F, Blanco-Prieto M (2010) Lipid nanoparticles in biomedicine. In: Nalwa HS (ed) Encyclopedia of nanoscience and nanotechnology. American Scientific Publishers, USA

    Google Scholar 

  • Domb A (1993) Lipsopheres for controlled delivery of substances. Google Patents

    Google Scholar 

  • Fang J-Y, Fang C-L, Liu C-H, Su Y-H (2008) Lipid nanoparticles as vehicles for topical psoralen delivery: solid lipid nanoparticles (SLN) versus nanostructured lipid carriers (NLC). Eur J Pharm Biopharm 70(2):633–640

    Article  CAS  PubMed  Google Scholar 

  • Gasco M (1993) Inventor method for producing solid lipid microspheres having a narrow size distribution. US patent US5250236

    Google Scholar 

  • Gasco M, Saettone M, Zara G (2003) Pharmaceutical compositions suitable for the treatment of ophthalmic diseases. Google Patents

    Google Scholar 

  • Jaafar-Maalej C, Elaissari A, Fessi H (2012) Lipid-based carriers: manufacturing and applications for pulmonary route. Expert Opin Drug Del 9(9):1111–1127

    Article  CAS  Google Scholar 

  • Jain A, Agarwal A, Majumder S, Lariya N, Khaya A, Agrawal H et al (2010) Mannosylated solid lipid nanoparticles as vectors for site-specific delivery of an anti-cancer drug. J Control Release 148(3):359–367

    Article  CAS  PubMed  Google Scholar 

  • Jenning V, Gohla S (2001) Encapsulation of retinoids in solid lipid nanoparticles (SLN). J Microencapsul 18(2):149–158

    Article  CAS  PubMed  Google Scholar 

  • Kawabata Y, Wada K, Nakatani M, Yamada S, Onoue S (2011) Formulation design for poorly water-soluble drugs based on biopharmaceutics classification system: Basic approaches and practical applications. Int J Pharm 420(1):1–10

    Article  CAS  PubMed  Google Scholar 

  • Liu J, Gong T, Fu H, Wang C, Wang X, Chen Q et al (2008) Solid lipid nanoparticles for pulmonary delivery of insulin. Int J Pharm 356(1–2):333–344

    Article  CAS  PubMed  Google Scholar 

  • Magenheim B, Levy M, Benita S (1993) A new in vitro technique for the evaluation of drug release profile from colloidal carriers-ultrafiltration technique at low pressure. Int J Pharm 94(1):115–123

    Article  CAS  Google Scholar 

  • Merisko-Liversidge E, Liversidge G (2008) Drug nanoparticles: formulating poorly water-soluble compounds. Toxicol Pathol 36(1):43–48

    Article  CAS  PubMed  Google Scholar 

  • Muchow M, Maincent P, Müller R (2008) Lipid nanoparticles with a solid matrix (SLN®, NLC®, LDC®) for oral drug delivery. Drug Dev Ind Pharm 34(12):1394–1405

    Article  CAS  PubMed  Google Scholar 

  • Müller R, Keck C (2004) Challenges and solutions for the delivery of biotech drugs—a review of drug nanocrystal technology and lipid nanoparticles. J Biotechnol 113(1–3):151–170

    Article  PubMed  Google Scholar 

  • Müller R, Lucks J (1996) Inventors; Arzneistoffträger aus festen lipidteilchen, feste lipidnanosphären (sln) patent EP0605497A1

    Google Scholar 

  • Müller R, Petersen R, Hommoss A, Pardeike J (2007) Nanostructured lipid carriers (NLC) in cosmetic dermal products. Adv Drug Deliver Rev 59(6):522–530

    Article  Google Scholar 

  • Müller R, Radtke M, Wissing S (2002) Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC) in cosmetic and dermatological preparations. Adv Drug Deliver Rev 54:131–155

    Article  Google Scholar 

  • Noack A, Hause G, Mäder K (2012) Physicochemical characterization of curcuminoid-loaded solid lipid nanoparticles. Int J Pharm 423:440–451

    Article  CAS  PubMed  Google Scholar 

  • Porter C, Trevaskis N, Charman W (2007) Lipids and lipid-based formulations: optimizing the oral delivery of lipophilic drugs. Nat Rev Drug Discov 6(3):231–248

    Article  CAS  PubMed  Google Scholar 

  • Reis C, Neufeld R, Ribeiro A, Veiga F (2006) Nanoencapsulation I Methods for preparation of drug-loaded polymeric nanoparticles. Nanomed Nanotechnol 2(1):8–21

    Article  CAS  Google Scholar 

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

    Article  CAS  PubMed  Google Scholar 

  • Saupe A, Wissing S, Lenk A, Schmidt C, Müller R (2005) Solid lipid nanoparticles (SLN) and nanostructured lipid carriers (NLC)—structural investigations on two different carrier systems. Bio-Med Mater Eng 15(5):393–402

    CAS  Google Scholar 

  • Schäfer-Korting M, Mehnert W, Korting H-C (2007) Lipid nanoparticles for improved topical application of drugs for skin diseases. Adv Drug Deliver Rev 59(6):427–443

    Article  Google Scholar 

  • Severino P, Andreani T, Macedo A, Fangueiro J, Santana M, Silva A et al (2012) Current state-of-art and new trends on lipid nanoparticles (SLN and NLC) for oral drug delivery. J Drug Delivery

    Google Scholar 

  • Souto E, Almeida A, Müller R (2007) Lipid nanoparticles (SLN, NLC) for cutaneous drug delivery: structure, protection and skin effects. J Biomed Nanotechnol 3(4):317–331

    Article  CAS  Google Scholar 

  • Speiser P (1986) inventor Lipid nano pellets as drug carriers for oral administration patent EP 0167825

    Google Scholar 

  • Sznitowska M, Gajewska M, Janicki S, Radwanska A, Lukowski G (2001) Bioavailability of diazepam from aqueous-organic solution, submicron emulsion and solid lipid nanoparticles after rectal administration in rabbits. Eur J Pharm Biopharm 52(2):159–163

    Article  CAS  PubMed  Google Scholar 

  • Sznitowska M, Janicki S, Gajewska M, Kulik M (2000) Investigation of diazepam lipospheres based on Witepsol and lecithin intended for oral or rectal delivery. Acta Pol Pharm 57:61–64

    CAS  PubMed  Google Scholar 

  • Videira M, Botelho M, Santos A, Gouveia L, de Lima J, Almeida A (2002) Lymphatic uptake of pulmonary delivered radiolabelled solid lipid nanoparticles. J Drug Target 10(8):607–613

    Article  CAS  PubMed  Google Scholar 

  • Waitzberg D, Torrinhas R, Jacintho T (2006) New parenteral lipid emulsions for clinical use. JPen-Parenter Enter 30(4):351–367

    Article  CAS  Google Scholar 

  • Washington C (1996) Stability of lipid emulsions for drug delivery. Adv Drug Deliver Rev 20(2–3):131–145

    Article  CAS  Google Scholar 

  • Westesen K (2000) Novel lipid-based colloidal dispersions as potential drug administration systems—expectations and reality. Colloid Polym Sci 278:608–619

    Article  CAS  Google Scholar 

  • Wissing S, Kayser O, Müller R (2004) Solid lipid nanoparticles for parenteral drug delivery. Adv Drug Deliver Rev 56(9):1257–1272

    Article  CAS  Google Scholar 

  • Wong H, Bendayan R, Rauth A, Wu X (2004) Development of solid lipid nanoparticles containing ionically complexed chemotherapeutic drugs and chemosensitizers. J Pharm Sci 93(8):1993–2008

    Article  CAS  PubMed  Google Scholar 

  • Wong H, Bendayan R, Rauth A, Wu X (2006a) Simultaneous delivery of doxorubicin and GG918 (Elacridar) by new polymer-lipid hybrid nanoparticles (PLN) for enhanced treatment of multidrug-resistant breast cancer. J Control Release 116(3):275–284

    Article  CAS  PubMed  Google Scholar 

  • Wong H, Bendayan R, Rauth A, Xue H, Babakhanian K, Wu X (2006b) A mechanistic study of enhanced doxorubicin uptake and retention in multidrug resistant breast cancer cells using a polymer-lipid hybrid nanoparticle (PLN) system. J Pharmacol Exp Ther 317:1372–1381

    Article  CAS  PubMed  Google Scholar 

  • Wong H, Rauth A, Bendayan R, Manias J, Ramaswamy M, Liu Z et al (2006c) A new polymer-lipid hybrid nanoparticle system increases cytotoxicity of Doxorubicin against multidrug-resistant human breast cancer cells Pharm Res. 23(7):1574–1585

    Google Scholar 

  • Wong H, Rauth A, Bendayan R, Wu X (2007) In vivo evaluation of a new polymer-lipid hybrid nanoparticle (PLN) formulation of doxorubicin in a murine solid tumor model. Eur J Pharm Biopharm 65(3):300–308

    Article  CAS  PubMed  Google Scholar 

  • Yang S, Lu L, Cai Y, Zhu J, Liang B, Yang C (1999) Body distribution in mice of intravenously injected camptothecin solid lipid nanoparticles and targeting effect on brain. J Control Release 59(3):299–307

    Article  CAS  PubMed  Google Scholar 

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Authors and Affiliations

  1. Department of Chemistry and Biotechnology, Swinburne University of Technology, PO Box 218, Hawthorn, Melbourne, VIC, 3122, Australia

    Rohan Shah, Daniel Eldridge, Enzo Palombo & Ian Harding

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  1. Rohan Shah
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  2. Daniel Eldridge
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  3. Enzo Palombo
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  4. Ian Harding
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Correspondence to Rohan Shah .

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Shah, R., Eldridge, D., Palombo, E., Harding, I. (2015). Introduction. In: Lipid Nanoparticles: Production, Characterization and Stability. SpringerBriefs in Pharmaceutical Science & Drug Development. Springer, Cham. https://doi.org/10.1007/978-3-319-10711-0_1

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  • DOI: https://doi.org/10.1007/978-3-319-10711-0_1

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  • Publisher Name: Springer, Cham

  • Print ISBN: 978-3-319-10710-3

  • Online ISBN: 978-3-319-10711-0

  • eBook Packages: MedicineMedicine (R0)

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