Phenylalanine-coupled solid lipid nanoparticles for brain tumor targeting
Source abstract
Abstract
The purpose of this study is to investigate the targeting potential of amino acid (phenylalanine)-coupled solid lipid nanoparticles (SLN) loaded with ionically complexed doxorubicin HCl (Dox). Ionic complexation was used to enhance the loading efficiency and release characteristics of water soluble form of Dox. l-Type amino acid transporters (LAT1) are highly expressed on blood brain barrier as well as on many brain cancer cells, thus targeting LAT1 using phenylalanine improved anticancer activity of prepared nanocarrier. The phenylalanine-coupled SLN were characterized by fourier transform infrared spectroscopy, scanning electron microscope, transmission electron microscopy, particle size, zeta potential, entrapment efficiency and in vitro release. The particle size of the resulting SLN was found to be in the range of 163.3 ± 5.2 to 113.0 ± 2.6 nm, with a slightly negative surface charge. In ex vivo study on C6 glioma cell lines, the cellular cytotoxicity of the SLN was highly increased when coupled with phenylalanine. In addition, stealthing sheath of PEG present on the surface of the SLN enhanced the cellular uptake of the SLN on C6 glioma cell line. Results of biodistribution and fluorescence studies clearly revealed that phenylalanine-coupled SLN could deliver high amount of drug into the brain tumor cells and showed the brain-targeting potential.
Source: openaire · Quality: candidate unverified · Source record ↗
Research context
OpenAlex topics: Amino Acid Enzymes and Metabolism · Molecular Sensors and Ion Detection · Lanthanide and Transition Metal Complexes
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
References (26)
Show source-provided references
1. Asano S, Kameyama M, Oura A, Morisato A, Sakai H, Tabuchi Y, Chairoungdua A, Endou H, Kanai Y (2007) l-type amino acid transporter-1 expressed in human astrocytomas, U343MGa. Biolog Pharm Bull 30:415–42210.1248/bpb.30.415 ↗
2. Be′duneaua A, Saulniera P, Benoita JP (2007) Active targeting of brain tumors using nanocarriers. Biomaterials 28:4947–496710.1016/j.biomaterials.2007.06.011 ↗
3. Behin A, H-X K, Carpentier AF, Delattre JY (2003) Primary brain tumours in adults. Lancet 361(9354):323–33110.1016/S0140-6736(03)12328-8 ↗
4. Boado RJ, Li JY, Nagaya M, Zhang C, Pardridge WM (1999) Selective expression of the large neutral amino acid transporter at the blood–brain barrier. Proc Natl Acad Sci U 21:79–84
5. Duelli R, Enerson BE, Gerhart DZ, Drewes LR (2000) Expression of large amino acid transporter LAT1 in rat brain endothelium. J Cereb Blood Flow Metab 11:1557–156210.1097/00004647-200011000-00005 ↗
6. Duneaua AB, Saulniera P, Benoit JP (2007) Active targeting of brain tumors using nanocarriers. Biomaterials 28:4947–496710.1016/j.biomaterials.2007.06.011 ↗
7. Freshney RI (1983) Culture of animal cells: a manual of basic technique. Alan R Liss, New York, p 112
8. Fundar`o A, Cavallib R, Bargonic A, Vighettob D, Zaraa GP, Gascob MR (2000) Non-stealth and stealth solid lipid nanoparticles (SLN) carrying doxorubicin: pharmacokinetics and tissue distribution after I V administration to rats. Pharmacol Res 42:338–342
9. Gupta Y, Jain A, Jain SK (2007) Transeferrin-conjugated solid lipid nanoparticles for enhanced delivery of quinine dihydrocholride to the brain. J Pharm Pharmacology 59:1–610.1211/jpp.59.7.0004 ↗
10. Jain A, Agarwal A, Majumder S, Lariya N, Khaya A, Agrawal H, Majumdar S, Agrawal GP (2010) Mannosylated solid lipid nanoparticles as vectors for site-specific delivery of an anti-cancer drug. J Controlled Release 148(3):359–36710.1016/j.jconrel.2010.09.003 ↗
11. Kageyama T, Nakamura M, Matsuo A, Yamasaki Y, Takakura Y, Hashida M, Kanai Y, Naito M, Tsuruo T, Minato N, Shimohama S (2000) The 4F2hc/LAT1 complex transports l-DOPA across the blood–brain barrier. Brain Res 879:115–12110.1016/S0006-8993(00)02758-X ↗
12. Kaur IP, Bhandari R, Bhandari S, Kakkar V (2008) Potential of solid lipid nanoparticles in brain targeting. J Control Rel 127:97–10910.1016/j.jconrel.2007.12.018 ↗
13. Lin R, Ng LS, Wang CH (2005) In vitro study of anticancer drug doxorubicin in PLGA-based microparticles. Biomaterials 26:4476–448510.1016/j.biomaterials.2004.11.014 ↗
14. Ling V (1992) p-glycoprotein and resistance to anticancer drugs. Cancer 69:2603–260910.1002/1097-0142(19920515)69:10<2603::AID-CNCR2820691034>3.0.CO;2-E ↗
15. Miglietta A, Cavalli R, Bocca C, Gabriel L, Gasco MR (2000) Cellular uptake and cytotoxicity of solid lipid nanospheres (SLN) incorporating doxorubicin or paclitaxel. Int J Pharm 210:61–6710.1016/S0378-5173(00)00562-7 ↗
16. Misra A, Ganesh S (2003) Drug delivery to the central nervous system: a review. J Pharm Pharm Sci 6:252–273
17. Moore A, Basilion JP, Chiocca EA, Weissleder R (1998) Measuring transferring receptor gene expression by NMR imaging. Biochim Biophys Acta 1402:239–24910.1016/S0167-4889(98)00002-0 ↗
18. Rautio J, Laine K, (2008) Gynther M Enhanced brain drug delivery and targeting. Pharma Tech Europe
19. Reddy LH, Murthy RSR (2004) Pharmacokinetics and biodistribution studies of doxorubicin loaded poly (butyl cyanoacrylate) nanoparticles synthesized by two different techniques. Biomed Pap 148:161–16610.5507/bp.2004.029 ↗
20. Reddy LH, Meda N, Murthy RSR (2005) Rapid and sensitive HPLC method for the estimation of doxorubicin in dog blood—the silver nitrate artifac. Acta Pharm 55:81–91
21. Schoepf U, Marecos E, Melder R, Jain R, Weissleder R (1998) Intracellular magnetic labeling of lymphocytes for in vivo trafficking studies. Biotechniques 24:64210.2144/98244rr01 ↗
22. Schubert MA, Goymann CCM (2003) Solvent injection as a new approach for manufacturing lipid nanoparticles evaluation of the method and process parameters. Eur J Pharm Biopharm 55:125–13110.1016/S0939-6411(02)00130-3 ↗
23. Siekmann B, Westesen K (1994) Melt-homogenized solid lipid nanoparticles stabilized by the nonionic surfactant tyloxapol I Preparation and particle size determination. Pharm Pharmacol Lett 3:194–197
24. Storm G, Belliot SO, Daemen T, Lasic DD (1995) Surface modification of nanoparticles to oppose uptake by the mononuclear phagocyte system. Adv Drug Deliv Rev 17:31–4810.1016/0169-409X(95)00039-A ↗
25. Weissleder R, Cheng HC, Bogdanova A, Bogdanova A Jr (1997) Magnetically labeled cells can be detected by MR imaging. J Magn Reson Imaging 7:258–26310.1002/jmri.1880070140 ↗
26. Wong HL, Bendayan R, Rauth AM, Xiao YW (2004) Development of solid lipid nanoparticles containing ionically complexed chemotherapeutic drugs and chemosensitizers. J Pharm Sci 93(8):1993–200810.1002/jps.20100 ↗