การประยุกต์ใช้กรดไขมันทางเภสัชกรรม
DOI:
https://doi.org/10.69598/tbps.14.1.1-11คำสำคัญ:
กรดไขมัน, การประยุกต์ใช้, เภสัชกรรมบทคัดย่อ
กรดไขมันใช้เป็นส่วนประกอบของผลิตภัณฑ์ได้หลายชนิด เช่น อาหาร เครื่องสำอาง และยา ปัจจุบันมีการนำกรดไขมันมาใช้ทางเภสัชกรรมด้วย เนื่องจากสมบัติที่หลากหลายของสารกลุ่มนี้ ได้แก่ สมบัติทางเภสัชวิทยา เช่น ฤทธิ์ในการต้านเชื้อจุลชีพ การป้องกันการขยายตัวและปกป้องโครงสร้างเนื้อเยื่อต่อมลูกหมาก สมบัติทางเคมีฟิสิกส์บางประการของกรดไขมันสามารถช่วยปรับสมบัติต่าง ๆ ของตำรับ หรือตัวยาได้ เช่น การเพิ่มการละลาย การเพิ่มการดูดซึมและการซึมผ่าน การเพิ่มความคงตัวของตัวยาหรือระบบนำส่งยา การเพิ่มประสิทธิผลเชิงคลินิกและการควบคุมการปลดปล่อยสาร ปัจจัยที่ส่งผลกระทบต่อสมบัติของผลิตภัณฑ์ที่เตรียมจากกรดไขมัน ได้แก่ วิธีการขึ้นรูป ส่วนประกอบในตำรับ เอนไซม์ไลเปส และจุดหลอมเหลว ด้วยสมบัติของกรดไขมันที่มีความเข้ากันได้กับร่างกายและมีความเป็นพิษที่ต่ำ จึงทำให้สารนี้มีความน่าสนใจนำมาประยุกต์ใช้ทางเภสัชกรรม
เอกสารอ้างอิง
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18. Quintavalle U, Voinovich D, Perissutti B, Serdoz F, Grassi M. Theoretical and experimental characterization of stearic acid -based sustained release devices obtained by hot melt co-extrusion. J Drug Deliv Sci Technol. 2007;17:415-20.
19. Wang PY. The reliability of a compressed mixture of insulin and palmitic acid to sustain a reduction in hyperglycaemia in rodents. Trans Am Soc Artif Intern Organs. 1987;33:319–22.
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21. Li M, Zahi MR, Yuan Q, Tian F, Liang H. Preparation and stability of astaxanthin solid lipid nanoparticles based on stearic acid. Eur J Lipid Sci Technol. 2016;118:592-602.
22. Arouri A, Lauritsen KE, Nielsen HL, Mouritsen OG. Effect of fatty acids on the permeability barrier of model and biological membranes. Chem Phys Lipids. 2016;200:139–46.
23. Han HK, Amidon GL. Targeted prodrug design to optimize drug delivery. AAPS PharmSci. 2000;2(1):a6.
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25. Kandula MM, KumarKB S, Palanichamy S, Rampal A. Discovery and preclinical development of a novel prodrug conjugate of mesalamine with eicosapentaenoic acid and caprylic acid for the treatment of inflammatory bowel diseases. Int Immunopharmacol. 2016;40:443–51.
26. Huan M, Cui H, Teng Z, Zhang B, Wang J, Liu X, et al. In vivo anti-tumor activity of a new doxorubicin conjugate via -Linolenic Acid. Biosci Biotechnol Biochem. 2012;76:1577-9.
27. Yuan L, Wang J, Shen WC. Reversible lipidization prolongs the pharmacological effect, plasma duration, and liver retention of octreotide. Pharm Res. 2005:22:220–7
.
28. Killen BU, Corrigan OI. Factors influencing drug release from stearic acid based compacts. Int J Pharm. 2001;228:189–98.
29. Killen BU, Corrigan OI. Effect of soluble filler on drug release from stearic acid based compacts. Int J Pharm. 2006;316:47-51.
30. Vervaeck A, Monteyne T, Siepmann F, Boone MN, Hoorebeke LV, Beer TD, et al. Fatty acids for controlled release applications: a comparison between prilling and solid lipid extrusion as manufacturing techniques. Eur J Pharm Biopharm. 2015;97:173–84.
31. Xie S, Zhu L, Dong Z, Wang X, Wang Y, Li X, et al. Preparation, characterization and pharmacokinetics of enrofloxacin-loaded solid lipid nanoparticles: Influences of fatty acids. Colloids Surf B Biointerfaces. 2011;83:382–7.
32. Reynisdottir S, Dauzats M, Thörne A, Langin D. Comparison of hormone-sensitive lipase activity in visceral and subcutaneous human adipose tissue. J Clin Endocrinol Metab. 1997;82:4162–6.
33. Ruge T, Sukonina V, Myrnäs T, Lundgren M, Eriksson JW, Olivecrona G. Lipoprotein lipase activity/mass ratio is higher in omental than in subcutaneous adipose tissue. Eur J Clin Invest. 2006;6:16–21.
34. Coppack SW, Jensen MD, Miles JM. In vivo regulation of lipolysis in humans. J Lipid Res. 1994;5:177–93.
35. Schwab M, McGoverin CM, Gordon KC, Winter G, Rades T, Myschik J, et al. Studies on the lipase-induced degradation of lipid-based drug delivery systems. Part II – Investigations on the mechanisms leading to collapse of the lipid structure. Eur J Pharm Biopharm. 2013;84:456–63.
36. Kingsbury KJ, Paul S, Crossley A, Morgan DM. The fatty acid composition of human depot fat. Biochem J. 1961;78:541-50.
37. Elmadfa I, Kornsteiner M. Fats and fatty acid requirements for adults. Ann Nutr Metab. 2009;55:56–75.
38. Phadke DS, Keeney MP, Norris DA. Evaluation of batch-to-batch and manufacturer-to-manufacturer variability in the physical properties of talc and stearic acid. Drug Dev Ind Pharm. 1994;20:859–71.
39. Burdock GA, Carabin IG. Safety assessment of myristic acid as a food ingredient. Food Chem Toxicol. 2007;45:517–29.
40. Guse C, Koennings S, Maschke A, Hacker M, Becker C, Schreiner S, et al. Biocompatibility and erosion behavior of implants made of triglycerides and blends with cholesterol and phospholipids. Int J Pharm. 2006;314:153-60.
2. Pohl CH, Kock JLF, Thibane VS. Antifungal free fatty acids: a review. In: Mendez-Vilaz A, editor. Science against microbial pathogens: communicating current research and technological advances. Badajoz: Formatex Research Center; 2011. p.61-71.
3. Yang D, Pornpattananangkul D, Nakatsuji T, Chan M, Carson D, Huang CM, et al. The antimicrobial activity of liposomal lauric acid against Propionibacterium acnes. Biomaterials. 2009;30:6035–40.
4. Loftsson T, Iliveska B, Asgrimsdottir GM, Ormarsson OT, Stefansson E. Fatty acids from marine lipids: biological activity, formulation and stability. J Drug Deliv Sci Technol. 2016;34:71-5.
5. Babu SVV, Veeresh B, Patil AA, Warke YB. Lauric acid and myristic acid prevent testosterone induced prostatic hyperplasia in rats. Eur J Pharmacol. 2010;626:262–5.
6. Imai T, Nodomi K, Shameem M, Matsumoto H, Satoh T, Otagiri M. Mutual effect of egg albumin and fatty acids on bioavailability of dl-α-tocopherol. Int J Pharm. 1997;155:45–52.
7. Kossena GA, Charman WN, Boyd BJ, Porter CJH. A novel cubic phase of medium chain lipid origin for the delivery of poorly water soluble drugs. J Control Release. 2004;99:217–29.
8. Hochman J, Artursson P. Mechanisms of absorption enhancement and tight junction regulation. J Control Release. 1994;29:253–67.
9. Raoof AA, Chiu P, Ramtoola Z, Cumming IK, Teng C, Weinbach SP, et al. Oral bioavailability and multiple dose tolerability of an antisense oligonucleotide tablet formulated with sodium caprate. J Pharm Sci. 2004;93:1431–9.
10. Lane ME. Skin penetration enhancers. Int J Pharm. 2013;447:12-21.
11. Wang MY, Yang YY, Heng PWS. Skin permeation of physostigmine from fatty acids-based formulations: evaluating the choice of solvent. Int J Pharm. 2005;290:25–36.
12. Jenning V, Gysler A, Schäfer-Korting M, Gohla SH. Vitamin A loaded solid lipid nanoparticles for topical use: occlusive and drug targeting to the upper skin. Eur J Pharm Biopharm. 2000;49:211-8.
13. Mohl S, Winter G. Continuous release of rh-interferon
-2a from triglyceride implants: storage stability of the dosage forms. Pharm Dev Technol. 2006;11:103–10.
14. Zhang Q, Yie G, Li Y, Yang Q, Nagai T. Studies on the cyclosporin A loaded stearic acid nanoparticles. Int J Pharm. 2000;200:153–9.
15. Silva CO, Rijo P, Molpeceres J, Figueiredo IV, Ascensão L, Fernandes AS, et al. Polymeric nanoparticles modified with fatty acids encapsulating betamethasone for anti-inflammatory treatment. Int J Pharm. 2015;493:271–84.
16. Grassi M, Voinovich D, Franceschinis E, Perissutti B, Grcic JF. Theoretical and experimental study on theophylline release from stearic acid cylindrical delivery systems. J Control Release. 2003;92:275–89.
17. Monteyne T, Adriaensens P, Brouckaert D, Remon JP, Vervaet C, Beer TD. Stearic acid and high molecular weight PEO as matrix for the highly water soluble metoprolol tartrate incontinuous twin-screw melt granulation. Int J Pharm. 2016;512:158–67.
18. Quintavalle U, Voinovich D, Perissutti B, Serdoz F, Grassi M. Theoretical and experimental characterization of stearic acid -based sustained release devices obtained by hot melt co-extrusion. J Drug Deliv Sci Technol. 2007;17:415-20.
19. Wang PY. The reliability of a compressed mixture of insulin and palmitic acid to sustain a reduction in hyperglycaemia in rodents. Trans Am Soc Artif Intern Organs. 1987;33:319–22.
20. Yoo HS, Choi H-K, Park TG. Protein–fatty acid complex for enhanced loading and stability within biodegradable nanoparticles. J Pharm Sci. 2001;90:194-201.
21. Li M, Zahi MR, Yuan Q, Tian F, Liang H. Preparation and stability of astaxanthin solid lipid nanoparticles based on stearic acid. Eur J Lipid Sci Technol. 2016;118:592-602.
22. Arouri A, Lauritsen KE, Nielsen HL, Mouritsen OG. Effect of fatty acids on the permeability barrier of model and biological membranes. Chem Phys Lipids. 2016;200:139–46.
23. Han HK, Amidon GL. Targeted prodrug design to optimize drug delivery. AAPS PharmSci. 2000;2(1):a6.
24. Zaro JL. Lipid-based drug delivery carriers for prodrugs to enhance drug delivery. AAPS J. 2015;17:83–92.
25. Kandula MM, KumarKB S, Palanichamy S, Rampal A. Discovery and preclinical development of a novel prodrug conjugate of mesalamine with eicosapentaenoic acid and caprylic acid for the treatment of inflammatory bowel diseases. Int Immunopharmacol. 2016;40:443–51.
26. Huan M, Cui H, Teng Z, Zhang B, Wang J, Liu X, et al. In vivo anti-tumor activity of a new doxorubicin conjugate via -Linolenic Acid. Biosci Biotechnol Biochem. 2012;76:1577-9.
27. Yuan L, Wang J, Shen WC. Reversible lipidization prolongs the pharmacological effect, plasma duration, and liver retention of octreotide. Pharm Res. 2005:22:220–7
.
28. Killen BU, Corrigan OI. Factors influencing drug release from stearic acid based compacts. Int J Pharm. 2001;228:189–98.
29. Killen BU, Corrigan OI. Effect of soluble filler on drug release from stearic acid based compacts. Int J Pharm. 2006;316:47-51.
30. Vervaeck A, Monteyne T, Siepmann F, Boone MN, Hoorebeke LV, Beer TD, et al. Fatty acids for controlled release applications: a comparison between prilling and solid lipid extrusion as manufacturing techniques. Eur J Pharm Biopharm. 2015;97:173–84.
31. Xie S, Zhu L, Dong Z, Wang X, Wang Y, Li X, et al. Preparation, characterization and pharmacokinetics of enrofloxacin-loaded solid lipid nanoparticles: Influences of fatty acids. Colloids Surf B Biointerfaces. 2011;83:382–7.
32. Reynisdottir S, Dauzats M, Thörne A, Langin D. Comparison of hormone-sensitive lipase activity in visceral and subcutaneous human adipose tissue. J Clin Endocrinol Metab. 1997;82:4162–6.
33. Ruge T, Sukonina V, Myrnäs T, Lundgren M, Eriksson JW, Olivecrona G. Lipoprotein lipase activity/mass ratio is higher in omental than in subcutaneous adipose tissue. Eur J Clin Invest. 2006;6:16–21.
34. Coppack SW, Jensen MD, Miles JM. In vivo regulation of lipolysis in humans. J Lipid Res. 1994;5:177–93.
35. Schwab M, McGoverin CM, Gordon KC, Winter G, Rades T, Myschik J, et al. Studies on the lipase-induced degradation of lipid-based drug delivery systems. Part II – Investigations on the mechanisms leading to collapse of the lipid structure. Eur J Pharm Biopharm. 2013;84:456–63.
36. Kingsbury KJ, Paul S, Crossley A, Morgan DM. The fatty acid composition of human depot fat. Biochem J. 1961;78:541-50.
37. Elmadfa I, Kornsteiner M. Fats and fatty acid requirements for adults. Ann Nutr Metab. 2009;55:56–75.
38. Phadke DS, Keeney MP, Norris DA. Evaluation of batch-to-batch and manufacturer-to-manufacturer variability in the physical properties of talc and stearic acid. Drug Dev Ind Pharm. 1994;20:859–71.
39. Burdock GA, Carabin IG. Safety assessment of myristic acid as a food ingredient. Food Chem Toxicol. 2007;45:517–29.
40. Guse C, Koennings S, Maschke A, Hacker M, Becker C, Schreiner S, et al. Biocompatibility and erosion behavior of implants made of triglycerides and blends with cholesterol and phospholipids. Int J Pharm. 2006;314:153-60.
ดาวน์โหลด
เผยแพร่แล้ว
2018-09-19
รูปแบบการอ้างอิง
Chantadee, T., Lertsuphovanit, N., & Phaechamud, T. (2018). การประยุกต์ใช้กรดไขมันทางเภสัชกรรม. ไทยไภษัชยนิพนธ์, 14(1), 1–11. https://doi.org/10.69598/tbps.14.1.1-11
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