Nanostructured lipid carriers: A platform to lipophilic drug for oral bioavailability enhancement
Lipid based drug delivery system such as Solid lipid nanoparticle (SLN) and Nanostructured lipid carriers (NLC) are among the most promising drug delivery system used in many industries such as food, pharmaceuticals and cosmetics industries. Over the last few years, new constituents of lipids have developed and investigated for enhancement of bioavailability. The present manuscript is an attempt on solving the concerned uncertainty with efficacious peroral administration of hydrophobic drugs through fabricating new lipid formulations, NLC. NLC, the second-generation lipid carrier is usually composed of solid lipids and liquid lipids together in a system. This mixing causes depression in melting point of substrates and converts the mixture into solid form at body temperature and termed as NLC. NLC shows a high drug loading with minimum drug expulsion. The unique advantages of NLC over SLN and Lipid-drug conjugates (LDC) are increased capacity of drug loading, avoidance of drug expulsion. This manuscript gives detailed information on definitions and simple way of production methods, new approaches in formulation of NLC and it also highlights how NLC improves bioavailability of bioactive molecules through peroral route and its future perspective as a pharmaceutical carrier. It also gives idea about the supremacy of NLC over other lipid-based system.
Keywords: Bioavailability; Lipids; Lipophilic drugs; Nanostructured lipid carriers; Solid lipid nanoparticle.
2. Khan S, Baboota S, Ali J, Khan S, Narang RS, Narang JK, Nanostructured lipid carriers: An emerging platform for improving oral bioavailability of lipophilic drugs, International Journal of Pharmaceutical Investigation, 2015; 5(4):182-191.
3. Puri A, Loomis K, Smith B, Lee JH, Yavlovich A, Heldman E, et al, Lipid-Based Nanoparticles as Pharmaceutical Drug Carriers: From Concepts to Clinic, Critical Reviews in Therapeutic Drug Carrier Systems, 2009; 26(6):523-580.
4. Rajabi M, Mousa SA, Lipid Nanoparticles and their Application in Nanomedicine, Current Pharmaceutical Biotechnology, 2016; 17:662-672.
5. Muchow M, Maincent P, Muller RH, Lipid Nanoparticles with a Solid Matrix (SLN®, NLC®, LDC®) for Oral Drug Delivery, Drug Development and Industrial Pharmacy, 2008; 34(12):1394-1405.
6. Das S, Chaudhury A, Recent advances in lipid nanoparticle formulations with solid matrix for oral drug delivery, American Association of Pharmaceutical Scientists Pharm Sci Tech, 2011; 12(1):62-76.
7. Olbrich C, Gessner A, Schroder W, Kayser O, Muller RH, Lipid–drug conjugate nanoparticles of the hydrophilic drug diminazene-cytotoxicity testing and mouse serum adsorption, Journal of Controlled Release, 2004; 96(3):425-435.
8. Das RJ, Baishya K, Pathak K, Recent advancement of lipid drug conjugate as nanoparticulate drug delivery system, International research journal of pharmacy, 2013; 4(1):73-78.
9. Radtke M, Souto EB, Muller RH, Nanostructured Lipid Carriers: a novel generation of solid lipid drug carriers, Pharmaceutical Technology Europe, 2005; 17(4):45–50.
10. Cavalli R, Caputo O, Gasco MR, Solid lipospheres of doxorubicin and Idarubicin, International Journal of Pharmaceutics, 1993; 89:R9–R12.
11. Sarangi MK, Padhi S, Solid lipid nanoparticles–a review, Journal of Critical Reviews, 2016; 3(3):5-12.
12. Patel DK, Tripathy S, Nair SK, Kesharwani R, Nanostructured lipid carrier (NLC) a modern approach for topical delivery: A review. World journal of pharmacy and pharmaceutical sciences, 2013; 2(3):921-938.
13. Tej K, Moin A, Gowda DV, Karunakar A, Patel NP, Kamal SS, Nanostructured lipid carrier based drug delivery system, Journal of Chemical and Pharmaceutical Research, 2016; 8(2):627-643.
14. Kamble MS, Vaidya KK, Bhosale AV, Chaudhari PD, Solid lipid nanoparticles and Nanostructured lipid carriers- An overview, International Journal of Pharmaceutical and Chemical Science, 2012; 2(4):681- 691.
15. Anthony AA, Momoh MA and Builders PF, Lipid nanoparticulate drug delivery systems: A revolution in dosage form design and development, http://dx.doi.org/10.5772/50486.
16. Hussain MM, Intestinal lipid absorption and lipoprotein formation, Current opinion in lipidology, 2014; 25(3):200-6.
17. Seong KK, Cheol SH, Sang HK, Sun JY, Comparison between ZnO films grown by atomic layer deposition using H2 O or O3 as oxidant, Thin Solid Films, 2005; 478(1-2):103-108.
19. Reddy LHV, Murthy RSR, Lymphatic transport of orally administered drugs, Indian Journal of Experimental Biology, 2002; 40:1097-1109.
20. Yostawonkul J, Surassmo S, Iempridee T, Pimtong W, Suktham K, Sajomsang W, Gonil P, Ruktanonchai UR, Surface modification of nanostructure lipid carrier (NLC) by oleoyl-quaternized-chitosan as a mucoadhesive nanocarrier, Colloids and Surfaces B: Biointerfaces, 2017;149:301-311. https://doi.org/10.1016/j.colsurfb.2016.09.049
21. Ozgura U, Alivov YI, Liu C, Tekeb A, Reshchikov MA, A comprehensive review of ZnO materials and devices, Journal of Applied Physics, 2005; 98:041301.
22. Banerjee D, Lao JY, Wang DZ, Huang JY, Ren ZF, Large-quantity free-standing ZnO nanowires, Applied Physics Letters, 2003; 83: 2061.
23. Karuppasamy A, Subrahmanyam A, Effect of electron bombardment on the properties of ZnO thin films, Materials Letters, 2007; 61(4-5):1256-1259.
24. Pearton SJ, Norton DP, Ip K, Heo YW, Steiner T, Recent progress in processing and properties of ZnO, Progress in Materials Science, 2005; 50(3):293-340.
25. Natarajan J, Karri V, Anindita D, Nanostructured Lipid Carrier (NLC): A Promising Drug Delivery System, Global Journal of Nanomedicine, 2017; 1(5):001-006. DOI: 10.19080/GJN.2017.01.555575.
26. Nautyal U, Kaur S, Singh R, Singh S, Devi A, Nanostructure Lipid Carrier (NLC): the new generation of lipid nanoparticles, Asian Pacific journal of health sciences, 2015; 2(2):76-93.
27. Yang CR, Zhao XL, Hu HY, Li KX, Sun X, Li L, et al., Preparation, Optimization and Characteristic of Huperzine A Loaded Nanostructured Lipid Carriers, Chemical & pharmaceutical bulletin, 2010; 58(5):656-661.
28. Oldrich C, Bakowski U, Lehr CM, et al., Cationic solid- lipid nanoparticles can efficiently bind and transfect plasmid DNA, Journal of Controlled Release, 2001; 77:345-55.
29. Zur M ühlen A, Schwarz C, Mehnert W, Solid lipid nanoparticles (SLN) for controlled drug delivery – drug release and release mechanism, European journal of pharmaceutics and biopharmaceutics, 1998; 45:149-155.
30. Gasco MR, Method for producing solid lipid microspheres having a narrow size distribution.1993; US Pat. No. 5250236.
31. Chaturvedi PS, Vimal Kumar, Production Techniques of Lipid Nanoparticles: A Review, Research Journal of Pharmaceutical, Biological and Chemical Sciences. 2012; 3(3):525-541.
32. B. Heurtault, P. Saulnier, B. Pech, J. E. Proust, J.P. Benoit, A novel phase inversion-based process for the preparation of lipid nanocarriers, Pharmaceutical research, 2006; 19(6):875–880.
33. Reithmeier H, Hermann J, Gopferich A, Lipid microparticles as a parenteral controlled release device for peptides, Journal of Controlled Release, 2001; 73:339-350.
34. Eldem T, Speiser P, Hincal A, Optimization of spray-dried and congealed lipid microparticles and characterization of their surface morphology by scanning electron microscopy, Pharmaceutical research, 1991; 8:47-54.
35. Jain SK, Agrawal GP, Jain NK, A novel calcium silicate based microspheres of repaglinide: in vivo investigations, Journal of Controlled Release, 2006; 113:111-116.
36. Date AA, Vador N, Jagtap A, Nagarsenker MS, Lipid nanocarriers (GeluPearl) containing amphiphilic lipid Gelucire 50/13 as a novelstabilizer: fabrication, characterization and evaluation for oral drug delivery, Nanotechnology, 2011; 22:275102
37. Qi S, Marchaud D, Craig DQ, An investigation into the mechanism of dissolution rate enhancement of poorly water-soluble drugs from spray chilled gelucire 50/13 microspheres, Journal of pharmaceutical sciences, 2010; 99:262-74.
38. Patel RJ, Patel ZP, Formulation Optimization and Evaluation of Nanostructured Lipid Carriers Containing Valsartan, International Journal of Pharmaceutical Sciences and Nanotechnology, 2013; 6(2):2077-2086.
39. Fang JY, Chen CC, Tsai TH, Huang ZR, Effects of lipophilic emulsifiers on the oral administration of lovastatin from nanostructured lipid carriers: Physicochemical characterization and pharmacokinetics, European Journal of Pharmaceutics and Biopharmaceutics, 2010; 74(3):474-482.
40. Ko S, Suh S, Choe J, Choi KO, Positively charged nanostructured lipid carriers and their effect on the dissolution of poorly soluble drugs. Molecules, 2016; 21(5):672-684.
41. Zhou J, Zhou D, Improvement of oral bioavailability of lovastatin by using nanostructured lipid carriers, Drug design development and therapy, 2015; 9:5269-5275.
42. Ko S, Aditya NP, Shim M, Lee I, Lee Y, Im MH, Curcumin and Genistein Coloaded Nanostructured Lipid Carriers: In vitro Digestion and Antiprostate Cancer Activity, Journal of agricultural and food chemistry, 2013; 61:1878-1883.
43. Yin J, Hou Y, Yin Y, Song X, Selenium-coated nanostructured lipid carriers used for oral delivery of berberine to accomplish a synergic hypoglycemic effect, International journal of nanomedicine, 2017; 12:8671-8680.
44. Shah NV, Seth AK, Balaraman R, Aundhia CJ, Maheshwari RA, Parmar GR, Nanostructured lipid carriers for oral bioavailability enhancement of raloxifene: Design and in vivo study, Journal of Advanced Research, 2016; 7(3):423-434.
45. Thatipamula RP, Yamsani MR, Palem CR, Gannu R, Mudra gada S, Formulation and in vitro characterization of domperidone loaded solid lipid nanoparticles and nanostructured lipid carriers, DARU Journal of Pharmaceutical Sciences, 2011; 19(1):23-32.
46. Gadad AP, Tigadi SG, Mallappa P, Dandagi PM, Mastiholimath VS, Bolmal UB. Rosuvastatin Loaded Nanostructured Lipid Carrier: For Enhancement of Oral Bioavailability, Indian Journal of Pharmaceutical Education and Research, 2016; 50(4):605-611.
47. Velmurugan R, Selvamuthukumar S, Development and optimization of ifosfamide nanostructured lipidcarriers for oral delivery using response surface methodology, Applied nanoscience, 2016; 6:159-173.
48. Tian C, Asghar S, Wu Y, Chen Z, Jin X, Yin L, Huang L, Ping Q, Xiao Y, Improving intestinal absorption and oral bioavailability of curcumin via taurocholic acid-modified nanostructured lipid carriers, International Journal of Nanomedicine, 2017; 12:7897-7911.
49. Shangguan M, Lu Y, Qi J, Han J, Tian Z, Xie Y, Hu F, Yuan H, Wu W, Binary lipids based nanostructured lipid carriers for improved oral bioavailability of silymarin, Journal of biomaterials applications, 2013. https://doi.org/10.1177/0885328213485141
50. Mitrea E, Ott C, Meghea A, New Approaches on the Synthesis of Effective Nanostructured Lipid Carriers, Revista De Chimie, 2014; 65(1):50-55. doi: http://www.revistadechimie.ro
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