Enteric-coated sustained-release nanoparticles by coaxial electrospray: preparation, characterization, and in vitro evaluation
Source abstract
Abstract
Enteric-coated formulations can delay the release of drugs until they have passed through the stomach. However, high concentration of drugs caused by rapidly released in the small intestine leads to the intestinal damage, and frequent administration would increase the probability of missing medication and reduce the patient compliance. To solve the above-mentioned problems, aspirin-loaded enteric-coated sustained-release nanoparticles with core–shell structure were prepared via one-step method using coaxial electrospray in this study. Eudragit L100-55 as pH-sensitive polymer and Eudragit RS as sustained-release polymer were used for the outer coating and inner core of the nanoparticles, respectively. The maximum loading capacity of nanoparticles was 23.66 % by changing the flow rate ratio of outer/inner solutions, and the entrapment efficiency was nearly 100 %. Nanoparticles with core–shell structure were observed via fluorescence microscope and transmission electron microscope. And pH-sensitive and sustained drug release profiles were observed in the media with different pH values (1.2 and 6.8). In addition, mild cytotoxicity in vitro was detected, and the nanoparticles could be taken up by Caco-2 cells within 1.0 h in cellular uptake study. These results indicate that prepared enteric-coated sustained-release nanoparticles would be a more safety and effective carrier for oral drug delivery.
Source: openaire · Quality: candidate unverified · Source record ↗
Research context
OpenAlex topics: Electrohydrodynamics and Fluid Dynamics · Microfluidic and Capillary Electrophoresis Applications · Electrospun Nanofibers in Biomedical Applications
SciVX discovery tags are terminology-based. OpenAlex topics are source-provided classifications.
References (44)
Show source-provided references
1. Ajun W, Yan S, Li G, Huili L (2009) Preparation of aspirin and probucol in combination loaded chitosan nanoparticles and in vitro release study. Carbohydr Polym 75(4):566–57410.1016/j.carbpol.2008.08.019 ↗
2. Alhnan MA, Kidia E, Basit AW (2011) Spray-drying enteric polymers from aqueous solutions: a novel, economic, and environmentally friendly approach to produce pH-responsive microparticles. Eur J Pharm Biopharm 79(2):432–43910.1016/j.ejpb.2011.03.015 ↗
3. Aubrey-Medendorp C, Parkin S, Li T (2008) The confusion of indexing aspirin crystals. J Pharm Sci 97(4):1361–136710.1002/jps.21055 ↗
4. Behrendt JM, Nagel D, Chundoo E, Alexander LM, Dupin D, Hine AV, Bradley M, Sutherland AJ (2013) Synthesis and characterization of dual-functionalized core–shell fluorescent microspheres for bioconjugation and cellular delivery. PLoS ONE 8(3):e5071310.1371/journal.pone.0050713 ↗
5. Chauhan MJ, Patel SA (2012) A concise review on sustained drug delivery system and its opportunities. Am J PharmTech Res 2(2):227–238
6. Choonara YE, Pillay V, Ndesendo VM, du Toit LC, Kumar P, Khan RA, Murphy CS, Jarvis D-L (2011) Polymeric emulsion and crosslink-mediated synthesis of super-stable nanoparticles as sustained-release anti-tuberculosis drug carriers. Colloid Surface B 87(2):243–25410.1016/j.colsurfb.2011.05.025 ↗
7. Chung Y-I, Tae G, Hong Yuk S (2006) A facile method to prepare heparin-functionalized nanoparticles for controlled release of growth factors. Biomaterials 27(12):2621–262610.1016/j.biomaterials.2005.11.043 ↗
8. Cramer JA, Glassman M, Rienzi V (2002) The relationship between poor medication compliance and seizures epilepsy. Behaviour 3(4):338–342
9. Dammann H, Burkhardt F, Wolf N (1999) Enteric coating of aspirin significantly decreases gastroduodenal mucosal lesions. Aliment Pharmacol Ther 13(8):1109–111410.1046/j.1365-2036.1999.00588.x ↗
10. Davis SS (2005) Formulation strategies for absorption windows. Drug Discov Today 10(4):249–25710.1016/S1359-6446(04)03351-3 ↗
11. Faivre J, Faivre M, Lery N, Ducluzeau R, Moulinier B, Paliard P (2009) Aspirin and gastrointestinal bleeding. Digestion 19(3):218–22010.1159/000198348 ↗
12. Farinha A, Bica A, Pais J, Toscano M, Tavares P (1999) Bioequivalence evaluation of two omeprazole enteric-coated formulations in humans. Eur J Pharm Sci 7(4):311–31510.1016/S0928-0987(98)00043-8 ↗
13. Felber AE, Dufresne M-H, Leroux J-C (2012) pH-sensitive vesicles, polymeric micelles, and nanospheres prepared with polycarboxylates. Adv Drug Delivery Rev 64(11):979–99210.1016/j.addr.2011.09.006 ↗
14. Grafahrend D, Jungbecker P, Seide G, Leonards H, Gries T, Möller M, Klee D (2010) Development and optimization of an electrospraying device for the continuous collection of nano- and microparticles. Open Chem Biomed Methods J 3:1–910.2174/1875038901003010001 ↗
15. Hao S, Wang B, Wang Y, Zhu L, Wang B, Guo T (2013) Preparation of Eudragit L 100-55 enteric nanoparticles by a novel emulsion diffusion method. Colloids Surf B 108(1):127–13310.1016/j.colsurfb.2013.02.036 ↗
16. Hawthorne A, Mahida Y, Cole A, Hawkey C (1991) Aspirin-induced gastric mucosal damage: prevention by enteric-coating and relation to prostaglandin synthesis. Br J Clin Pharmacol 32(1):77–8310.1111/j.1365-2125.1991.tb05616.x ↗
17. Higuchi K, Umegaki E, Watanabe T, Yoda Y, Morita E, Murano M, Tokioka S, Arakawa T (2009) Present status and strategy of NSAIDs induced small bowel injury. J Gastroenterol 44(9):879–88810.1007/s00535-009-0102-2 ↗
18. Hosny EA (1996) Formulation and comparative evaluation of bioadhesive containing diclofenac sodium and commercial enteric coated tablets in vitro and in dogs. Int J Pharm 133(1):149–15310.1016/0378-5173(95)04426-4 ↗
19. Hosny EA, Al-Shora HI, Elmazar M (2002) Oral delivery of insulin from enteric-coated capsules containing sodium salicylate: effect on relative hypoglycemia of diabetic beagle dogs. Int J Pharm 237(1):71–7610.1016/S0378-5173(02)00024-8 ↗
20. Huynh DP, Im GJ, Chae SY, Lee KC, Lee DS (2009) Controlled release of insulin from pH/temperature-sensitive injectable pentablock copolymer hydrogel. J Controlled Release 137(1):20–2410.1016/j.jconrel.2009.02.021 ↗
21. Kendall RA, Alhnan MA, Nilkumhang S, Murdan S, Basit AW (2009) Fabrication and in vivo evaluation of highly pH-responsive acrylic microparticles for targeted gastrointestinal delivery. Eur J Pharm Sci 37(3):284–29010.1016/j.ejps.2009.02.015 ↗
22. Lee Y-H, Bai M-Y, Chen D-R (2011) Multidrug encapsulation by coaxial tri-capillary electrospray. Colloid Surface B 82(1):104–11010.1016/j.colsurfb.2010.08.022 ↗
23. Li H, Zhao X, Ma Y, Zhai G, Li L, Lou H (2009) Enhancement of gastrointestinal absorption of quercetin by solid lipid nanoparticles. J Controlled Release 133(3):238–24410.1016/j.jconrel.2008.10.002 ↗
24. Lim CH, Mullins ME (2012) Synthesis of core–shell biopolymer particles using coaxial electrospray. In: MRS Proceedings. Cambridge University Press, Cambridge10.1557/opl.2012.877 ↗
25. Liu F, Lizio R, Meier C, Petereit H-U, Blakey P, Basit AW (2009) A novel concept in enteric coating: a double-coating system providing rapid drug release in the proximal small intestine. J Controlled Release 133(2):119–12410.1016/j.jconrel.2008.09.083 ↗
26. Loscertales IG, Barrero A, Guerrero I, Cortijo R, Marquez M, Ganan-Calvo A (2002) Micro/nano encapsulation via electrified coaxial liquid jets. Science 295(5560):1695–169810.1126/science.1067595 ↗
27. McCarron P, Woolfson AD, Keating SM (2000) Sustained release of 5-fluorouracil from polymeric nanoparticles. J Pharm Pharmacol 52(12):1451–145910.1211/0022357001777658 ↗
28. Modi SA, Gaikwad P, Bankar V, Pawar S (2011) Sustained release drug delivery system: a review. Int J Pharm Res Dev 2:147–160
29. Okuda T, Yoshida N, Takagi T, Handa O, Kokura S, Ichikawa H, Naito Y, Yoshikawa T (2008) CV-11974, angiotensin II type I receptor antagonist, reduces the severity of indomethacin-induced rat enteritis. Dig Dis Sci 53(3):657–66310.1007/s10620-007-9931-0 ↗
30. Pan X, Ju J, Zhan Y, Wu D (2010) Preparation and fluorescence characteristics of amido-functionalized dual-fluorescent microspheres with core/shell structure. Macromol Chem Phys 211(21):2347–235510.1002/macp.201000243 ↗
31. Panyam J, Labhasetwar V (2003) Biodegradable nanoparticles for drug and gene delivery to cells and tissue. Adv Drug Delivery Rev 55(3):329–34710.1016/S0169-409X(02)00228-4 ↗
32. Pignatello R, Bucolo C, Ferrara P, Maltese A, Puleo A, Puglisi G (2002) Eudragit RS100®nanosuspensions for the ophthalmic controlled delivery of ibuprofen. Eur J Pharm Sci 16(1):53–6110.1016/S0928-0987(02)00057-X ↗
33. Satoh H, Takeuchi K (2012) Management of NSAID/aspirin-induced small intestinal damage by GI-sparing NSAIDs, anti-ulcer drugs and food constituents. Curr Med Chem 19(1):82–8910.2174/092986712803413980 ↗
34. Shahani K, Swaminathan SK, Freeman D, Blum A, Ma L, Panyam J (2010) Injectable sustained release microparticles of curcumin: a new concept for cancer chemoprevention. Cancer Res 70(11):4443–445210.1158/0008-5472.CAN-09-4362 ↗
35. Shen Y, Chen J, Liu Q, Feng C, Gao X, Wang L, Zhang Q, Jiang X (2011) Effect of wheat germ agglutinin density on cellular uptake and toxicity of wheat germ agglutinin conjugated PEG–PLA nanoparticles in Calu-3 cells. Int J Pharm 413(1):184–19310.1016/j.ijpharm.2011.04.026 ↗
36. Sonaje K, Lin K-J, Tseng MT, Wey S-P, Su F-Y, Chuang E-Y, Hsu C-W, Chen C-T, Sung H-W (2011) Effects of chitosan-nanoparticle-mediated tight junction opening on the oral absorption of endotoxins. Biomaterials 32(33):8712–872110.1016/j.biomaterials.2011.07.086 ↗
37. Soppimath KS, Aminabhavi TM, Kulkarni AR, Rudzinski WE (2001) Biodegradable polymeric nanoparticles as drug delivery devices. J Controlled Release 70(1):1–2010.1016/S0168-3659(00)00339-4 ↗
38. Sun Z, Zussman E, Yarin AL, Wendorff JH, Greiner A (2003) Compound core–shell polymer nanofibers by co-electrospinning. Adv Mater 15(22):1929–193210.1002/adma.200305136 ↗
39. Toorisaka E, Hashida M, Kamiya N, Ono H, Kokazu Y, Goto M (2005) An enteric-coated dry emulsion formulation for oral insulin delivery. J Controlled Release 107(1):91–9610.1016/j.jconrel.2005.05.022 ↗
40. van Breemen RB, Li Y (2005) Caco-2 cell permeability assays to measure drug absorption. Expert Opin Drug Met 1(2):175–18510.1517/17425255.1.2.175 ↗
41. Vane LM, Zang GM (1997) Effect of aqueous phase properties on clay particle zeta potential and electro-osmotic permeability: Implications for electro-kinetic soil remediation processes. J Hazard Mater 55(1):1–2210.1016/S0304-3894(97)00010-1 ↗
42. Walker J, Robinson J, Stewart J, Jacob S (2007) Does enteric-coated aspirin result in a lower incidence of gastrointestinal complications compared to normal aspirin? Interact Cardiovasc and Thorac Surg 6(4):519–52210.1510/icvts.2007.155788 ↗
43. Wang Y, Zhang Y, Wang B, Cao Y, Yu Q, Yin T (2013) Fabrication of core–shell micro/nanoparticles for programmable dual drug release by emulsion electrospraying. J Nanopart Res 15(6):1–12
44. Zhang S, Kawakami K, Yamamoto M, Masaoka Y, Kataoka M, Yamashita S, Sakuma S (2011) Coaxial electrospray formulations for improving oral absorption of a poorly water-soluble drug. Mol Pharm 8(3):807–81310.1021/mp100401d ↗