Submicron lipid emulsions: A versatile platform for drug delivery

Current Drug Metabolism

Volumn 16, Issue 3, 2015, Pages 211-220

  Zhang, Xingwang ^a   Wu, Baojian ^a  

^a JINAN UNIVERSITY   (China)

Author keywords

ADME; Application; Lipid emulsions; Manufacture; Quality assessment

Indexed keywords

ANTINEOPLASTIC AGENT; LIPID EMULSION; DRUG CARRIER; EMULSION; LIPID;

ARTICLE; CENTRIFUGATION; DIFFUSION; DISPERSION; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG MANUFACTURE; DRUG STABILITY; EMULSION; FREEZE DRYING; GENE TARGETING; HUMAN; PARENTERAL NUTRITION; PARTICLE SIZE; QUALITY CONTROL; SOLUBILIZATION; ANIMAL; CHEMISTRY; DRUG ADMINISTRATION ROUTE; INTRAVENOUS DRUG ADMINISTRATION;

ANIMALS; DRUG ADMINISTRATION ROUTES; DRUG CARRIERS; EMULSIONS; HUMANS; INJECTIONS, INTRAVENOUS; LIPIDS; QUALITY CONTROL;

EID: 84940880027     PISSN: 13892002     EISSN: 18755453     Source Type: Journal    
DOI: 10.2174/138920021603150812124221     Document Type: Article

References (83)

1. Hippalgaonkar, K.; Majumdar, S.; Kansara, V. Injectable lipid emulsions-advancements, opportunities and challenges. AAPS Pharm. Sci. Tech., 2010, 11(4), 1526-1540.
2. Azeem, A.; Rizwan, M.; Ahmad, F.J.; Khan, Z.I.; Khar, R.K.; Aqil, M.; Talegaonkar, S. Emerging role of microemulsions in cosmetics. Recent Pat. Drug Deliv. Formul., 2008, 2(3), 275-289.
3. Wang, J; Cui, Y.; Tang, X. Chemical stability of teniposide in aqueous and parenteral lipid emulsions. Drug Dev. Ind. Pharm., 2009, 35(4), 508-513.
4. Simovic, S; Hui, H.; Song, Y.; Davey, A.K.; Rades, T.; Prestidge, C.A. An oral delivery system for indomethicin engineered from cationic lipid emulsions and silica nanoparticles. J. Control. Release, 2010, 143(3), 367-373.
5. Ades, A; Carvalho, J.P.; Graziani, S.R.; Amancio, R.F.; Souen, J.S.; Pinotti, J.A.; Maranhao, R.C. Uptake of a cholesterol-rich emulsion by neoplastic ovarian tissues. Gynecol. Oncol., 2001, 82(1), 84-87.
6. Xiong, F; Wang, H.; Chen, Y.J.; Geng, K.K.; Gu, N.; Zhu, J.B. Characterization, biodistribution and targeting evaluation of breviscapine lipid emulsions following intravenous injection in mice. Drug Deliv., 2011, 18(2), 159-165.
7. Zheng, J; Tang, Y.; Sun, M.; Zhao, Y.; Li, Q.; Zhou, J.; Wang, Y. Characterization, pharmacokinetics, tissue distribution and antitumor activity of honokiol submicron lipid emulsions in tumorburdened mice. Pharmazie, 2013, 68(1), 41-46.
8. Prabhakar, K; Afzal, S.M.; Kumar, P.U.; Rajanna, A.; Kishan, V. Brain delivery of transferrin coupled indinavir submicron lipid emulsions-pharmacokinetics and tissue distribution. Colloids Surf. B. Biointerfaces, 2011, 86(2), 305-313.
9. Kandadi, P; Syed, M.A.; Goparaboina, S.; Veerabrahma, K. Brain specific delivery of pegylated indinavir submicron lipid emulsions. Eur. J. Pharm. Sci., 2011, 42(4), 423-432.
10. Schultz, S; Wagner, G.; Urban, K.J. Ulrich, High-pressure homogenization as a process for emulsion formation. Chem. Eng. Technol., 2004, 27(4), 361-368.
11. Angare, D; Giri, T.; Tripathi, D.K.; Alexander, A.; Ajazuddin. Unexplored Areas and New Findings in Lipid Emulsion Serving as a Potential Drug Carrier for Lipophilic Drugs: A Review. Trends Med. Res., 2012, 7(1-24).
12. Maan, A.A; Schroën, K.; Boom, R. Spontaneous droplet formation techniques for monodisperse emulsions preparation - Perspectives for food applications. J. Food Eng., 2011, 107(3-4), 334-346.
13. Floury, J; Desrumaux, A.; Lardières, J. Effect of high-pressure homogenization on droplet size distributions and rheological properties of model oil-in-water emulsions. Innov. Food Sci. Emerg., 2000, 1(2), 127-134.
14. Hayes, M.G; Fox, P.F.; Kelly, A.L. Potential applications of high pressure homogenisation in processing of liquid milk. J. Dairy Res., 2005, 72(1), 25-33.
15. Eggers, R. Industrial High Pressure Applications: Processes, Equipment, and Safety, Wiley-VCH, Weinheim, 2012.
16. Marquez, A.L.; Wagner, J.R. Rheology of Cream-like Emulsions Prepared with Soybean Milk and Low Trans Vegetable Fat. J. Am. Oil Chem. Soc., 2012, 89(10), 1857-1865.
17. Charcosset, C.; Limayem, I.; Fessi, H. The membrane emulsification process-a review. J. Chem. Technol. Biotechnol., 2004, 79(3), 209-218.
18. Jiang, S.P.; He, S.N.; Li, Y.L.; Feng, D.L.; Lu, X.Y.; Du, Y.Z.; Yu, H.Y.; Hu, F.Q.; Yuan, H. Preparation and characteristics of lipid nanoemulsion formulations loaded with doxorubicin. Int. J Nanomedicine, 2013, 8(3141-3150).
19. Bollam, S.; P. Kandadi, S.S. Apte, K. Veerabrahma, Development of indinavir submicron lipid emulsions loaded with lipoamino acids- in vivo pharmacokinetics and brain-specific delivery. AAPS PharmSciTech, 2011, 12(1), 422-430.
20. Tenambergen, F.; Maruiama, C.H.; Mader, K. Dual asymmetric centrifugation as an alternative preparation method for parenteral fat emulsions in preformulation development. Int. J. Pharm., 2013, 447(1-2), 31-37.
21. Porter, C.J.H.; Trevaskis, N.L.; Charman, W.N. Lipids and lipidbased formulations: optimizing the oral delivery of lipophilic drugs. Nat. Rev. Drug Discov., 2007, 6(3), 231-248.
22. Renou, C.; Carriere, F.; Ville, E.; Grandval, P.; Joubert-Collin, M.; Laugier, R. Effects of lansoprazole on human gastric lipase secretion and intragastric lipolysis in healthy human volunteers. Digestion, 2001, 63(4), 207-213.
23. Bauer, E.; Jakob, S.; Mosenthin, R. Principles of Physiology of Lipid Digestion Asian-Aust. J. Anim. Sci., 2005, 18(2), 282-295.
24. Ring, A.; Pohl, J.; Volkl, A.; Stremmel, W. Evidence for vesicles that mediate long-chain fatty acid uptake by human microvascular endothelial cells. J. Lipid Res., 2002, 43(12), 2095-2104.
25. Gan, L.; Wang, J.; Jiang, M.; Bartlett, H.; Ouyang, D.; Eperjesi, F.; Liu, J.; Gan, Y. Recent advances in topical ophthalmic drug delivery with lipid-based nanocarriers. Drug Discov. Today, 2013, 18(5- 6), 290-297.
26. Duvvuri, S.; Majumdar, S.; Mitra, A.K. Role of metabolism in ocular drug delivery. Curr. Drug Metab., 2004, 5(6), 507-515.
27. Kurihara, A.; Shibayama, Y.; Kasuya, A.; Ikeda, M.; Hisaoka, M. Species variation in pharmacokinetics and opsonization of palmitoyl rhizoxin (RS-1541) incorporated in lipid emulsions. J. Drug Target., 1998, 5(6), 491-505.
28. Longmire, M.; Choyke, P.L.; Kobayashi, H. Clearance properties of nano-sized particles and molecules as imaging agents: considerations and caveats. Nanomedicine, 2008, 3(5), 703-717.
29. Nelson, R.H.; Edgerton, D.S.; Basu, R.; Roesner, J.C.; Cherrington, A.D.; Miles, J.M. Triglyceride uptake and lipoprotein lipasegenerated fatty acid spillover in the splanchnic bed of dogs. Diabetes, 2007, 56(7), 1850-1855.
30. Nguyen, P.; Leray, V.; Diez, M.; Serisier, S.; Le Bloc'h, J.; Siliart, B.; Dumon, H. Liver lipid metabolism. J. Anim. Physiol. Anim. Nutr. (Berl.), 2008, 92(3), 272-283.
31. Kamijo, A.; Sugaya, T.; Hikawa, A.; Okada, M.; Okumura, F.; Yamanouchi, M.; Honda, A.; Okabe, M.; Fujino, T.; Hirata, Y.; Omata, M.; Kaneko, R.; Fujii, H.; Fukamizu, A.; Kimura, K. Urinary excretion of fatty acid-binding protein reflects stress overload on the proximal tubules. Am. J. Pathol., 2004, 165(4), 1243-1255.
32. Dowhan, W. The role of phospholipids in cell function, in: W.G. Richard (Ed.) Advances in Lipobiology, JAI, 1997, pp. 79-107.
33. De Maria, L.; Vind, J.; Oxenboll, K.M.; Svendsen, A.; Patkar, S. Phospholipases and their industrial applications. Appl. Microbiol. Biotechnol., 2007, 74(2), 290-300.
34. Reshetnyak, V.I. Physiological and molecular biochemical mechanisms of bile formation. World J. Gastroenterol., 2013, 19(42), 7341-7360.
35. Grindel, J.M.; Jaworski, T.; Piraner, O.; Emanuele, R.M.; Balasubramanian, M. Distribution, metabolism, and excretion of a novel surface-active agent, purified poloxamer 188, in rats, dogs, and humans. J. Pharm. Sci., 2002, 91(9), 1936-1947.
36. Ren, T.Y.; Cong, L.; Wang, Y.Q.; Tang, Y.L.; Tian, B.; Lin, X.; Zhang, Y.; Tang, X. Lipid emulsions in parenteral nutrition: current applications and future developments. Expert Opin. Drug Del., 2013, 10(11), 1533-1549.
37. Bullimore, D.W. A comparison of the incidence of injection pain with two different diazepam formulations-Valium and Diazemuls. Clin. Ther., 1982, 4(5), 367-368.
38. Zhan, Y.P.; Huang, X.E.; Cao, J.; Lu, Y.Y.; Wu, X.Y.; Liu, J.; Xu, X.; Xiang, J.; Ye, L.H. Clinical safety and efficacy of Kanglaite(R) (Coix Seed Oil) injection combined with chemotherapy in treating patients with gastric cancer. Asian Pac. J. Cancer Prev., 2012, 13(10), 5319-5321.
39. Zhao, Y.X.; Liu, D.X.; Liang, W.Q.; Ye, Z.W. In-vivo pharmacokinetics, tissue distribution and anti-tumour effect of hydroxycamptothecin delivered in oil-in-water submicron emulsions. J. Pharm. Pharmacol., 2012, 64(6), 783-791.
40. Lundberg, B.B.; Risovic, V.; Ramaswamy, M.; Wasan, K.M. A lipophilic paclitaxel derivative incorporated in a lipid emulsion for parenteral administration. J. Control. Release, 2003, 86(1), 93-100.
41. Li, Y.; Jin, W.; Yan, H.; Liu, H.; Wang, C. Development of intravenous lipid emulsion of vinorelbine based on drug-phospholipid complex technique. Int. J. Pharm., 2013, 454(1), 472-477.
42. Constantinides, P.P.; Tustian, A.; Kessler, D.R. Tocol emulsions for drug solubilization and parenteral delivery. Adv. Drug Del. Rev., 2004, 56(9), 1243-1255.
43. M, H.; P. M.; Aqther, A.; N. R.; B., P.K. Dry emulsion: A promising dosage form to deliver lipophilic drug molecules with improved stability and effectiveness. Indian J. Res. Pharm. Biotech., 2014, 1(1), 119-121.
44. Kararli, T.T.; Needham, T.E.; Griffin, M.; Schoenhard, G.; Ferro, L.J.; Alcorn, L. Oral delivery of a renin inhibitor compound using emulsion formulations. Pharm. Res., 1992, 9(7), 888-893.
45. Han, S.-f.; Yao, T.-t.; Zhang, X.-x.; Gan, L.; Zhu, C.; Yu, H.-z.; Gan, Y. Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: Effects of lipid composition and formulation. Int. J. Pharm., 2009, 379(1), 18-24.
46. Cho, H.T.; Salvia-Trujillo, L.; Kim, J.; Park, Y.; Xiao, H.; McClements, D.J. Droplet size and composition of nutraceutical nanoemulsions influences bioavailability of long chain fatty acids and Coenzyme Q10. Food Chem., 2014, 156(117-122).
47. Müller, R.H.; Schmidt, S.; Buttle, I.; Akkar, A.; Schmitt, J.; Brömer, S. SolEmuls®-novel technology for the formulation of i.v. emulsions with poorly soluble drugs. Int. J. Pharm., 2004, 269(2), 293-302.
48. Knibbe, C.A.; Voortman, H.J.; Aarts, L.P.; Kuks, P.F.; Lange, R.; Langemeijer, H.J.; Danhof, M. Pharmacokinetics, induction of anaesthesia and safety characteristics of propofol 6% SAZN vs propofol 1% SAZN and Diprivan-10 after bolus injection. Br. J. Clin. Pharmacol., 1999, 47(6), 653-660.
49. Ohmukai, O. Lipo-NSAID preparation. Adv. Drug Del. Rev., 1996, 20(2-3), 203-207.
50. Junghanns, J.U.; Buttle, I.; Muller, R.H.; Araujo, I.B.; Silva, A.K.A.; Egito, E.S.T. B.P.G.L. Damasceno, SolEmuls® technology: A way to overcome the drawback of parenteral administration of insoluble drugs. Pharm. Dev. Technol., 2007, 12(5), 437-445.
51. Shi, J.; Chen, X.; Gu, Y.; Hu, X.; Zhang, L., Li, Y.; Cai, C.; Tang, X. Preformulation and development of chemically stable lipid emulsions containing a novel taxane derivative, TM-2. Eur. J. Lipid Sci. Technol., 2014, 116(4), 486-496.
52. Marin-Quintero, D.; Fernandez-Campos, F.; Calpena-Campmany, A.C.; Montes-Lopez, M.J.; Clares-Naveros, B.; Del Pozo- Carrascosa, A. Formulation design and optimization for the improvement of nystatin-loaded lipid intravenous emulsion. J. Pharm. Sci., 2013, 102(11), 4015-4023.
53. Yi, S.W.; Yune, T.Y.; Kim, T.W.; Chung, H.; Choi, Y.W.; Kwon, I.C.; Lee, E.B.; Jeong, S.Y. A cationic lipid emulsion/DNA complex as a physically stable and serum-resistant gene delivery system. Pharm. Res., 2000, 17(3), 314-320.
54. Bruxel, F.; Cojean, S.; Bochot, A.; Teixeira, H.; Bories, C.; Loiseau, P.M.; Fattal, E. Cationic nanoemulsion as a delivery system for oligonucleotides targeting malarial topoisomerase II. Int. J. Pharm., 2011, 416(2), 402-409.
55. Fraga, M.; Bruxel, F.; Lagranha, V.L.; Teixeira, H.F.; Matte, U. Influence of phospholipid composition on cationic emulsions/DNA complexes: physicochemical properties, cytotoxicity, and transfection on Hep G2 cells. Int. J. Nanomed., 2011, 6(2213-2220).
56. Bivas-Benita, M.; Oudshoorn, M.; Romeijn, S.; van Meijgaarden, K.; Koerten, H.; van der Meulen, H.; Lambert, G.; Ottenhoff, T.; Benita, S.; Junginger, H.; Borchard, G. Cationic submicron emulsions for pulmonary DNA immunization. J. Control. Release, 2004, 100(1), 145-155.
57. Choi, B.Y.; Chung, J.W.; Park, J.H.; Kim, K.H.; Kim, Y.I.; Koh, Y.H.; Kwon, J.W.; Lee, K.H.; Choi, H.J.; Kim, T.W.; Kim, Y.J.; Chung, H.; Kwon, I.C.; Jeong, S.Y. Gene delivery to the rat liver using cationic lipid emulsion/DNA complex: comparison between intra-arterial, intraportal and intravenous administration. Korean J. Radiol., 2002, 3(3), 194-198.
58. Kang, H.S.; Jin, S.J.; Myung, C.S.; Hwang, S.J.; Park, J.S. Delivery of interleukin-18 gene to lung cancer cells using cationic emulsion. J. Drug Target., 2009, 17(1), 19-28.
59. Kim, T.W.; Chung, H.; Kwon, I.C.; Sung, H.C.; Shin, B.C.; Jeong, S.Y. Airway gene transfer using cationic emulsion as a mucosal gene carrier. J. Gene Med., 2005, 7(6), 749-758.
60. Zhang, X.; Wu, W. Ligand-mediated active targeting for enhanced oral absorption. Drug Discov. Today, 2014, 19(7), 898-904.
61. Ganta, S.; Talekar, M.; Singh, A.; Coleman, T.P.; Amiji, M.M. Nanoemulsions in translational research-opportunities and challenges in targeted cancer therapy. AAPS Pharm. Sci. Tech., 2014, 15(3), 694-708.
62. Petrenko, V. Evolution of phage display: from bioactive peptides to bioselective nanomaterials. Expert Opin. Drug Deliv., 2008, 5(8), 825-836.
63. Kim, S.H.; Kim, J.K.; Lim, S.J.; Park, J.S.; Lee, M.K.; Kim, C.K. Folate-tethered emulsion for the target delivery of retinoids to cancer cells. Eur. J. Pharm. Biopharm., 2008, 68(3), 618-625.
64. Guo, Y.; Liu, X.; Sun, X.; Zhang, Q.; Gong, T.; Zhang, Z. Mannosylated lipid nano-emulsions loaded with lycorine-oleic acid ionic complex for tumor cell-specific delivery. Theranostics, 2012, 2(11), 1104-1114.
65. Reddy, P.R.; Venkateswarlu, V. Pharmacokinetics and tissue distribution of etoposide delivered in long circulating parenteral emulsion. J. Drug Target., 2005, 13(10), 543-553.
66. Zhao, H.; Lu, H.; Gong, T.; Zhang, Z. Nanoemulsion loaded with lycobetaine-oleic acid ionic complex: physicochemical characteristics, in vitro, in vivo evaluation, and antitumor activity. Int. J. Nanomedicine, 2013, 8(1959-1973).
67. Alayoubi, A.; Alqahtani, S.; Kaddoumi, A.; Nazzal, S. Effect of PEG surface conformation on anticancer activity and blood circulation of nanoemulsions loaded with tocotrienol-rich fraction of palm oil. AAPS J., 2013, 15(4), 1168-1179.
68. Zhao, D.; Gong, T.; Fu, Y.; Nie, Y.; He, L.L.; Liu, J.; Zhang, Z.R. Lyophilized Cheliensisin A submicron emulsion for intravenous injection: characterization, in vitro and in vivo antitumor effect. Int. J. Pharm., 2008, 357(1-2), 139-147.
69. Chen, H.; Shi, S.; Zhao, M.; Zhang, L.; He, H.; Tang, X. A lyophilized etoposide submicron emulsion with a high drug loading for intravenous injection: preparation, evaluation, and pharmacokinetics in rats. Drug Dev. Ind. Pharm., 2010, 36(12), 1444-1453.
70. Yu, C.; Meng, J.; Chen, J.; Tang, X. Preparation of ergoloid mesylate submicron emulsions for enhancing nasal absorption and reducing nasal ciliotoxicity. Int. J. Pharm., 2009, 375(1-2), 16-21.
71. Vahabzadeh, M.; Moshiri, M.; Mohammadpour, A.H.; Hosseinzadeh, H. Promising effects of intravenous lipid emulsion as an antidote in acute tramadol poisoning. Reg. Anesth. Pain Med., 2013, 38(5), 425-430.
72. Gianella, A.; Jarzyna, P.A.; Mani, V.; Ramachandran, S.; Calcagno, C.; Tang, J.; Kann, B.; Dijk, W.J.; Thijssen, V.L.; Griffioen, A.W.; Storm, G.; Fayad, Z.A.; Mulder, W.J. Multifunctional nanoemulsion platform for imaging guided therapy evaluated in experimental cancer. ACS nano, 2011, 5(6), 4422-4433.
73. Gao, K.; Sun, J.; Liu, K.; Liu, X.; He, Z. Preparation and characterization of a submicron lipid emulsion of docetaxel: submicron lipid emulsion of docetaxel. Drug Dev. Ind. Pharm., 2008, 34(11), 1227-1237.
74. Han, S.F.; Yao, T.T.; Zhang, X.X.; Gan, L.; Zhu, C.; Yu, H.Z.; Gan, Y. Lipid-based formulations to enhance oral bioavailability of the poorly water-soluble drug anethol trithione: Effects of lipid composition and formulation. Int. J. Pharm., 2009, 379(1), 18-24.
75. Muller, R.H.; Schmidt, S.; Buttle, I.; Akkar, A.; Schmitt, J.; Bromer, S. SolEmuls-novel technology for the formulation of i.v. emulsions with poorly soluble drugs. Int. J. Pharm., 2004, 269(2), 293-302.
76. Kim, T.W.; Chung, H.; Kwon, I.C.; Sung, H.C.; Kang, T.H.; Han, H.D.; Jeong, S.Y. Induction of immunity against hepatitis B virus surface antigen by intranasal DNA vaccination using a cationic emulsion as a mucosal gene carrier. Mol. Cells, 2006, 22(2), 175- 181.
77. Liu, Y.; Lin, X.; Tang, X. Lipid emulsions as a potential delivery system for ocular use of azithromycin. Drug Dev. Ind. Pharm., 2009, 35(7), 887-896.
78. Nasr, M.; Nawaz, S.; Elhissi, A. Amphotericin B lipid nanoemulsion aerosols for targeting peripheral respiratory airways via nebulization. Int. J. Pharm., 2012, 436(1-2), 611-616.
79. Hou, H.W.; Bhagat, A.A.S.; Lee, W.C.; Huang, S.; Han, J.; Lim, C.T. Microfluidic Devices for Blood Fractionation. Micromachines- Basel, 2011, 2(3), 319-343.
80. Driscoll, D.F.; Ling, P.R.; Andersson, C.; Bistrian, B.R. Hepatic Indicators of Oxidative Stress and Tissue Damage Accompanied by Systemic Inflammation in Rats Following a 24-Hour Infusion of an Unstable Lipid Emulsion Admixture. JPEN J. Parenter. Enteral., 2009, 33(3), 327-335.
81. Mirtallo, J.M.; Dasta, J.F.; Kleinschmidt, K.C.; Varon, J. State of the art review: Intravenous fat emulsions: Current applications, safety profile, and clinical implications. Ann. Pharmacother., 2010, 44(4), 688-700.
82. Becvarova, I.; Saker, K.E.; Swecker, W.S.; Troy, G.C Jr. Peroxidative protection of parenteral admixture by D-alpha-tocopherol. Vet. Ther., 2005, 6(4), 280-290.
83. McCracken, M. Fat embolism after lipid emulsion infusion. Lancet, 1991, 337(8747), 983.