Solid Lipid Microparticles: Formulation, Preparation, Characterisation, Drug Release and Applications

[en] This review details the properties of solid lipid microparticles (SLMs): a promising drug carrier system that has been until now rather unexploited. First, the advantages of SLMs compared with other drug carrier systems are listed. Then an overview of SLM manufacturing compounds and techniques is presented. A detailed discussion of the characteristics of SLMs follows, and includes the determination of particle size distribution, the determination of SLM morphology, the solid-state analysis, the determination of SLM drug loading and the factors influencing it. The in vitro drug release studies that have been carried out so far and the parameters affecting them are also described. Some preliminary in vivo aspects (in vivo drug release studies, biocompatibility studies and in vivo fate) are also considered.

Disciplines :

Pharmacy, pharmacology & toxicology

Author, co-author :

Jaspart, Séverine ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique et magistrale

Piel, Géraldine ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique et magistrale

Delattre, Luc ; Université de Liège - ULiège > Département de pharmacie > Département de pharmacie

Evrard, Brigitte ; Université de Liège - ULiège > Département de pharmacie > Pharmacie galénique

Language :

English

Title :

Solid Lipid Microparticles: Formulation, Preparation, Characterisation, Drug Release and Applications

Publication date :

January 2005

Journal title :

Expert Opinion on Drug Delivery

ISSN :

1742-5247

eISSN :

1744-7593

Publisher :

Taylor & Francis, United Kingdom

Volume :

Issue :

Pages :

75-87

Peer reviewed :

Peer Reviewed verified by ORBi

Available on ORBi :

since 28 April 2010

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135 (4 by ULiège)

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3 (1 by ULiège)

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Scopus citations^®

155

Scopus citations^®
without self-citations

152

OpenCitations

123

Bibliography

MEHNERT W, MADER K: Solid lipid nanoparticles: production, characterization and applications. Adv. Drug Deliv. Rev. (2001) 47:165-196.
ZENG XM, MARTIN GP, MARRIOTT C: The controlled delivery of drugs to the lung. Int. J. Pharm. (1995):149-164.
BARRATT GM: Therapeutic applications of colloidal drug carriers. Pharm. Sci. Tecchnol Today (2000) 3(5):163-171.
SHARMA A, SHARMA US: Liposomes in drug delivery: Progress and limitations. Int. J. Pharm. (1997) 154(2):123-140.
MANOSROI A, KONGKANERAMIT L, MANOSROI J: Stability and transdermal absorption of topical amphotericin B liposome formulations. Int. J. Pharm. (2004) 270(1-2):279-286.
BRANNON-PEPPAS L: Recent advances on the use of biodegradable microparticles and nanoparticles in controlled drug delivery. Int. J. Pharm. (1995) 116(1):1-9.
RAVI KUMAR MNV. Nano and microparticles as controlled drug delivery devices. J. Pharm. Pharm. Sci. (2000) 3(2 ):234-258.
SOPPIMATH KS, AMINABHAVI TM, KULKARNI AR et al.: Biodegradable polymeric nanoparticles as drug delivery devices. J Control. Release (2001) 70(1-2):1-20.
ALLEMAN E, GURNY R, DOELKER E: Drug-loaded nanoparticles - preparation methods and drug targeting issues. Eur. J. Pharm. Biopharm. (1993) 39(5):173-191.
REITHMEIER H, HERRMANN J, GOPFERICH A: Development and characterization of lipid microparticles as a drug carrier for somatostatin. Int. J. Pharm. (2001) 218:133-143.
GUPTA PK, ADJEI AL: Modulated-release aerosol. In: Inhalation delivery of therapeutic peptides and proteins. Lung biology in health and disease. Gupta Pkadjei Al (Ed.), New York (2003):667-702.
DEL VALLE EMM: Cyclodextrins and their uses: a review. Process Biochemistry (2004) 39(9):1033-1046.
DUCHENE D, WOUESSIDJEWE D, PONCHEL G: Cyclodextrins and carrier systems. J. Control. Release (1999) 62(1-2): 263-268.
HU FQ, YUAN H, ZHANG HH et al.: Preparation of solid lipid nanoparticles with clobetasol propionate by a novel solvent diffusion method in aqueous system and physicochemical characterization. Int. J. Pharm. (2002) 239:121-128.
MULLER RH, MADER K, GOHLA S: Solid lipid nanoparticles (SLN) for controlled drug delivery- a review of the state of art. Eur. J. Pharm. Biopharm. (2000) 50:161-177.
SCHWARZ C, MEHNERT W: Solid lipid nanoparticles (SLN) for controlled drug delivery; drug incorporation and physicochemical characterization. J. Microencapsul. (1999) 16(2):205-213.
VENKATESWARLU V, MANJUNATH K: Preparation, characterization and in vitro release kinetics of clozapine solid lipid nanoparticles. J. Control. Release (2004) 95:627-638.
ZUR MUHLEN A, SCHWARZ C, MEHNERT W: Solid lipid nanoparticles (SLN) for controlled drug delivery- Drug release and release mechanism. Eur. J. Pharm. Biopharm. (1998) 45:149-155.
HOU D, XIE C, HUANG K et al: The production and characteristics of solid lipid nanoparticles (SLNs). Biomaterials (2003) 24(10):1781-1785.
SAVOLAINEN M, HERDER J, KHOO C et al.: Evaluation of polar lipid-hydrophilic polymer microparticles. Int. J. Pharm. (2003) 262(1-2):47-62.
PASSERINI N, PERISSUTTI B, ALBERTINI B et al.: Controlled release of verapamil hydrochloride from waxy microparticles prepared by spray congealing. J. Control. Release (2003) 88 2):263-275.
AKIYAMA Y, YOSHIOKA M, HORIBE H et al.: Novel oral controlled-release microspheres using polyglycerol esters of fatty acids. J. Control. Release (1993) 26(1):1-10.
RODRIGUEZ L, PASSERINI N, CAVALLARI C et al.: Description and preliminary evaluation of a new ultrasonic atomizer for spray-congealing processes. Int. J. Pharm. (1999) 183 2):133-143.
DEL CURTO MD, CHICCO D, D'ANTONIO M et al.: Lipid microparticles as sustained release system for a GnRH antagonist (Antide). J. Control. Release (2003) 89:297-310.
FREDERIKSEN HK, KRISTENSEN HG, PEDERSEN M: Solid lipid microparticle formulations of the pyrethroid gamma-cyhalothrin-incompatibility of the lipid and the pyrethroid and biological properties of the formulations. J. Control. Release (2003) 86:243-252.
DEMIREL M, YAZAN Y, MULLER RH et al.: Formulation and in vitro-in vivo evaluation of piribedil solid lipid micro- and nanoparticles. J. Microencapsul. (2001) 18(3):359-371.
SANNA V, KIRSCHVINK N, GUSTIN P et al.: Preparation and in vivo toxicity study of solid lipid microparticles as carrier for pulmonary administration. AAPS PharmSci Tech (2004) 5 2):Article 27.
ELDEM T, SPEISER P, HINCAL A: Optimization of spray-dried and congealed lipid micropellets and characterization of their surface morphology by scanning electron microscopy. Pharm. Res. (1991) 8 1):47-54.
BODMEIER R, WANG J, BHAGWATWAR H: Process and formulation variables in the preparation of wax microparticles by a melt dispersion technique. I. Oil-in-water technique for water-insoluble drugs. J. Microencapsul. (1992) 9(1):89-98.
BODMEIER R, WANG J, BHAGWATWAR H: Process and formulation variables in the preparation of wax microparticles by a melt dispersion technique. II. W/O/W multiple emulsion technique for water-soluble drugs. J. Microencapsul. (1992) 9(1):99-107.
REITHMEIER H, HERRMANN J, GOPFERICH A: Lipid microparticles as parenteral controlled release device for peptides. J. Control. Release (2001) 73:339-350.
ERNI C, SUARD C, FREITAS S et al.: Evaluation of cationic sold tipid microparticles as synthetic carriers for the targeted delivery of macromolecules to phagocytic antigen-presenting cells. Biomaterials (2004) 23:4667-4676.
REITHMEIER H, GOPFERICH A, HERRMANN J: Preparation and characterization of lipid microparticles containing insulin. Proceedings of the 2nd World Meeting APGI/APV. Paris, France (1998) 1079.
MASTERS DB, DOMB AJ: Liposphere local anesthetic timed-release for perineural site application. Pharm. Res. (1998) 15(7):1038-1045.
BENITA S, ZOUAI O, BENOIT JP: 5-Fluorouracil: carnauba wax microspheres for chemoembloization: An in vitro evaluation. J. Pharm. Sci. US (1986) 75(9):847-851.
PASSERINI N, PERISSUTI B, MONEGHINI M et al.: Characterization of carbamazepine-Gelucire 50/13 microparticles prepared by a spray-congealing process using ultrasounds. J. Pharm. Sci-US (2002) 91(3):699-707.
YENER G, INCEGUL T, YENER N: Importance of using solid lipid microspheres as carriers for UV filters on the example octyl methoxy cinnamate. Int. J. Pharm. (2003) 258:203-207.
GIANNOLA LI, DI STEFANO V, DE CARO V: White beeswax microspheres: a comparative in vitro evaluation of cumulative release of the anticancer agents fluorouracil and ftorafur. Pharmazie (1993) 48(2):123-126.
BRASSEUR S, AMIGHI K, MOES AJ: Evaluation of solid lipid microparticles for controlled delivery to the pulmonary tract. Proceedings of the 9th Forum of Pharmaceutical Sciences. Spa, Belgium (2000) 11.
MALAMATARIS S, PANAGOPOULOU A, HATZIPANTOU P: Controlled release from glycerol palmito-stearate matrices prepared by dry-heat granulation and compression at elevated temperature. Drug. Dev. Ind. Pharm. (1991) 17:1765-1777.
SAVOLAINEN M, KHOO C, GLAD H et al.: Evaluation of controlled-release polar lipid microparticles. Int. J. Pharm. (2002) 244:151-161.
CORTESI R, ESPOSITO E, LUCA G et al.: Production of lipospheres as carriers for bioactive compounds. Biomaterials (2002) 23(11):2283-2294.
MULLER RH, MEHNERT W, LUCKS JS et al.: Solid lipid nanoparticles (SLN) - an alternative colloidal carrier system for controlled drug delivery. Eur. J. Pharm. Biopharm. (1995) 41 1):62-69.
SUGIURA S, NAKAJIMA M, TONG J et al.: Preparation of monodispersed solid lipid microspheres using a microchannel emulsification technique. J. Colloid Interf. Sci. (2000) 227 95-103.
KAWAKATSU T, TRAGARDH G, TRAGARDH C: Production of W/O/W emulsions and S/O/W pectin microcapsules by microchannel emulsification. Colloid Surface A (2001) 189:257-264.
KILLEEN MJ: Spray drying and spray congealing of pharmaceuticals. In: Encyclopedia of Pharmaceutical Technology SWARBRICK J, BOYLAN JC (Ed.) (2000):207-221.
BEUSELINCK L, GOVERS G, POESEN J et al.: Grain-size analysis by laser diffractometry: comparison with the sieve-pipette method. CATENA (1998) 32(3-4):193-208.
WASHINGTON C: Particle Size Analysis in Pharmaceutics and Other Industries: Theory and Practice. (1992) ELLIS HORWOOD.
WYNN EJW. HOUNSLOW MJ: Coincidence correction for electrical-zone (Coulter-counter) particle size analysers. Powder Technology (1997) 93(2):163-175.
MARTIN A. Micromeritics. In: Physical Pharmacy. Lippincott, Williams & Wilkins, Baltimore (2004):423-452.
US Pharmacopeia National Formulary (1995):1822-1823.
GOFFIN MEYVIS ANALYTICAL & MEDICAL SYSTEMS: Workshop on Image Analysers from Malvern Instruments (2004).
HICKEY AJ: Methods of aerosol particle size characterization. In: Pharmaceutical Inhalation Aerosol Technology. Drugs and the pharmaceutical sciences. HICKEY AJ (Ed.). Marcel Dekker, New York (2004):345-385.
US Pharmacopeia National Formulary (1995):1760-1767
CARLI F, GARBASSI F: Characterization of drug loading in crospovidone by X-ray photoelectron spectroscopy. J. Pharm. Sci. (1985) 74(9):963-967.
VOINOVICH D, MONEGHINI M, PERISSUTTI B et al.: Preparation in high-shear mixer of sustained-release pellets by melt pelletisation. Int. J. Pharm. (2000) 203(1-2):235-244.
WESTESEN K, BUNJES H, KOCH MHJ: Physicochemical characterization of lipid nanoparticles and evaluation of their drug loading capacity and sustained release. J. Control. Release (1997) 48:223-23.
WESTESEN K, SIEKMANN B, KOCH MHJ: Investigations on the physical state of lipid nanoparticles by synchrotron radiation X-ray diffraction. Int. J. Pharm. (1993) 93(1-3):189-199.
ELDEM T, SPEISER P, ALTORFER H: Polymorphic behavior of sprayed lipid micropellets and its evaluation by differential scanning calorimetry and scanning electron microscopy. Pharm. Res. (1991) 8(2):178-184.
MARTIN A: Micromeritics. In: Physical Pharmacy: Physical Chemical Principles in the Pharmaceutical Sciences. Lea and Febiger, London (1993):423-449.
MARTIN A: Micromeritics. In: Physical Pharmacy. Lippincott, Williams & Wilkins, Baltimore (2004):30-36.
VITEZ IM, NEWMAN AW, DAVIDOVICH M et al.: The evolution of hot-stage microscopy to aid solid-state characterizations of pharmaceutical solids. Thermochimica Acta (1998) 324(1-2): 187-196.
KANEKO F, TASHIRO K, KOBAYASHI M: Polymorphic transformations during crystallization processes of fatty acids studied with FT-IR spectroscopy. J. Cryst. Growth (1999) 198-199 (Part 2): 1352-1359.
YAZAN Y, DEMIREL M, BUYUKKOROGLU B et al.: Solid lipid microparticle versus inclusion complex of piribedil. Proceedings of the European Conference on Drug Delivery and Pharmaceutical Technology 10-12 May, 2004. Seville, Spain (2004).
JASPART S, BODSON C, BERTHOLET P et al.: Solid lipid microparticles for administration by inhalation: optimisation of manufacturing parameters. Proceedings of the European Conference on Drug Delivery and Pharmaceutical Technology. 10-12 May, Seville, Spain (2004).
JASPART S, KIRSCHVINK N, CHIAP P et al.: Solid lipid microparticles for administration by inhalation: optimisation of manufacturing parameters and preliminary tolerance study. Proceedings 12th Forum of Pharmaceutical Sciences. 6-7 May, Blankenberge, Belgium (2004).
BLANCO-PRIETO MJ, BESSEGHIR K, ORSOLINI P et al.: Importance of the test medium for the release kinetics of a somatostatin analogue from poly(-lactide-co-glycolide) microspheres. Int. J. Pharm. (1999) 184(2):243-250.
WOO BH, KOSTANSKI JW, GEBREKIDAN S et al.: Preparation, characterization and in vivo evaluation of 120-day poly(-lactide) leuprolide microspheres. J. Control. Release (2001) 75 3):307-315.
OLBRICH C, MULLER RH: Enzymatic degradation of SLN-effect of surfactant and surfactant mixtures. Int. J. Pharm. (1999) 180 1):31-39.
OLBRICH C, KAYSER O, MULLER RH: Lipase degradation of Dynasan 114 and 116 solid lipid nanoparticles (SLN)-effect of surfactants, storage time and crystallinity. Int. J. Pharm. (2002) 237 1-2):119-128.