Samoemulgující systém (SEDDS) pro podání léčiva ibuprofen: hodnocení vzorků v podmínkách in vitro a in vivo
Authors:
Subhash Chandra Bose Penjuri; Saritha Damineni; Nagaraju Ravouru; Srikanth Reddy Poreddy
Published in:
Čes. slov. Farm., 2017; 66, 23-34
Category:
Original Articles
Overview
Cílem této studie bylo vyvinout samoemulgující systém (SEDDS) pro perorální podání těžce rozpustného léčiva ibuprofenu a zhodnotit jeho biologickou dostupnost. K určení fázového chování mikroemulzí a srovnání účinnosti různých směsí povrchově aktivní látky a oleje byly sestaveny fázové diagramy. Samoemulgující systémy ibuprofenu byly připraveny ze směsi Labrafilu M2125, Cremophoru RH40 a Plurol oleique. U připravených emulzí bylo hodnoceno jejich chování v podmínkách in vitro a in vivo. FTIR hodnocení nepotvrdilo žádnou interakci mezi léčivem a pomocnými látkami. DSC studie prokázaly, že léčivo je v systému solubilizováno. Vzorky byly dále hodnoceny na termodynamickou stabilitu, dispersibilitu, index lomu, viskozitu a bod zákalu. Připravené vzorky ukázaly negativní náboj částic vnitřní fáze, což ukazuje na jejich stabilitu. Systém optimalizovaného složení představoval mikroemulzi s velikostí vnitřní fáze 177,5 nm. Množství uvolněného léčiva v podmínkách in vitro bylo významně vyšší než u přípravku dostupného na trhu a čistého léčiva. Farmakodynamické studie optimalizované složení ukázala vyšší protizánětlivý účinek ve srovnání s přípravkem dostupným na trhu a čistým léčivem. Hodnoty AUC a Cmax po perorálním podání byly vyšší pro SEDDS s obsahem ibuprofenu ve srovnání s přípravkem dostupným na trhu. Dosažené výsledky naznačují, že SEDDS by mohl být užitečnou alternativou pro zvýšení biologické dostupnosti špatně rozpustných léčiv.
Klíčová slova:
ibuprofen • samoemulgující systém • fázový diagram • zeta potenciál • protizánětlivá aktivita
Sources
1. Quan D. Q., Xu G. X., Wu X. G. Studies on preparation and absolute bioavailability of a self-emulsifying system containing puerarin. Chem. Pharm. Bull. 2007; 55, 800–803.
2. Humberstone A. J., Charman W. N. Lipid-based vehicles for the oral delivery of poorly water soluble drugs. Adv. Drug. Deliv. Rev. 1997; 25, 103–128.
3. Gursoy R. N., Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed. Pharmacother. 2004; 58, 173–182.
4. Porter C. J., Charman W. N. Intestinal lymphatic drug transport: An update. Adv. Drug. Deliv. Rev. 2001; 50, 61–80.
5. Shah N. H., Carvajal M. T., Patel C. I., Infeld M. H., Malick A. W. Self-emulsifying drug delivery systems (SEDDS) with polyglycolyzed glycerides for improving in vitro dissolution and oral absorption of lipophilic drugs. Int. J. Pharm. 1994; 106, 15–23.
6. Pradeep Patil., Prasad Joshi., Anant Paradkar. Effect of formulation variables on preparation and evaluation of gelled self-emulsifying drug delivery system (SEDDS) of ketoprofen. AAPS. PharmSciTech. 2004; 5, 1–8.
7. Pouton C. W., Charman W. N. The potential of oily formulations for drug delivery to the gastro-intestinal tract. Adv. Drug. Deliv. Rev. 1997; 25, 1–2.
8. Pouton C. W. Formulation of self-emulsifying drug delivery systems. Adv. Drug. Deliv. Rev. 1997; 25, 47–58.
9. Kapsi S. G., Ayres J. W. Processing factors in development of solid solution formulation of itraconazole for enhancement of drug dissolution and bioavailability. Int. J. of Pharm. 2001; 229, 193–203.
10. Maeda T., Takenaka H., Yamahira Y., Noguchi T. Use of rabbits for GI drug absorption studies: Relationship between dissolution rate and bioavailability of griseofulvin tablets. J. Pharm. Sci. 1979; 68, 1286–1289.
11. Chiba Y., Kohri N., Iseki K., Miyazaki K. Improvement of dissolution and bioavailability for mebendazole, an agent for human echinococcosis, by preparing solid dispersion with polyethylene glycol. Chem. Pharm. Bull. 1991; 39, 2158–2160.
12. Prabagar Balakrishnan, Beom-Jin Lee, Dong Hoon Oh, Jong Oh Kim, Myung Ja Hong, Jun-Pil Jee, Jung Ae Kim, Bong Kyu Yoo, Jong Soo Wooa, Chul Soon Yong, Han-Gon Choia. Enhanced oral bioavailability of dexibuprofen by a novel solid self-emulsifying drug delivery system (SEDDS). Eur. J. Pharm. Biopharm. 2009; 72, 539–545.
13. Indian Pharmacopoeia, Ministry of Health and Family welfare, The Indian Pharmacopoeia commission, Ghaziabad, 6th edition., Vol I, 2010; 559–560.
14. Hong J. Y., Kim J. K., Song Y. K., Park J. S., Kim C. K. A new self-emulsifying formulation of itraconazole with improved dissolution and oral absorption. J. Control. Release. 2006; 110, 332–338.
15. Avachat A. M., Patel V. G. Self nanoemulsifying drug delivery system of stabilized ellagic acid–phospholipid complex with improved dissolution and permeability. Saudi. Pharm. J. 2015: 23, 276–289.
16. Shafiq-un-Nabi S., Shakeel F., Talegaonkar S., Ali J., Baboota S., Ahuja A., Khar R. K., Mushir A. Formulation development and optimization using nanoemulsion technique: A technical note. AAPS. PharmSciTech. 2007; 8, E1–E6.
17. Sheikh S., Shakeel F., Talegaonkar S., Ahmad F. J., Khar R.K., Ali M. Development and bioavailability assessment of ramipril nanoemulsion formulation. Eur. J. Pharm. Biopharm. 2007; 66, 227–243.
18. Khoo S. M., Humberstone A. J., Porter C. J., Edwards G. A., Charman W. N. Formulation design and bioavailability assessment of lipidic self-emulsifying formulations of halofantrine. Int. J. Pharm. 1998; 167, 155–164.
19. Patel D., Sawant K. K. Oral Bioavailability Enhancement of Acyclovir by Self Microemulsifying Drug Delivery Systems (SMEDDS). Drug. Dev. Ind. Pharm. 2007; 33, 1318–1326.
20. Ramadan E., Borg T. H., Abdelghani G. M., Saleh N. M. Formulation and evaluation of acyclovir microemulsions. Bull. Pharm. Sci. 2013; 36, 31–47.
21. Kallakunta V. R., Bandari S., Jukanti R., Veerareddy P. R. Oral self-emulsifying powder of lercanidipine hydrochloride: formulation and evaluation. Powder. Technol. 2012; 221, 375–382.
22. Taha E. I., Al-Saidan S., Samy A. M., Khan M. A. Preparation and in vitro characterization of self-nanoemulsified drug delivery system (SNEDDS) of all-trans-retinol acetate, Int. J. Pharm. 2004; 285, 109–119.
23. Nazzal S., Nutan M., Palamakula A., Shah R., Zaghloul A. A., Khan M. A. Optimization of a self-nanoemulsified tablet dosage form of Ubiquinone using response surface methodology: effect of formulation ingredients. Int. J. Pharm. 2002; 240, 103–114.
24. Cho H. J., Ku W. S., Termsarasab U., Yoon I., Chung C. W., Moon H. T., Kim D. D. Development of udenafil-loaded microemulsions for intranasal delivery: In vitro and in vivo evaluations. Int. J. Pharm. 2012; 423, 153–160.
25. Damineni Saritha., Penjuri Subhash Chandra Bose., Ravouru Nagaraju. Formulation and evaluation of self-emulsifying drug delivery system (SEDDS) of ibuprofen. Int. J. Pharm. Sci. Res. 2014; 5, 3511–3519.
26. Lichtenberger L. M., Romero J. J., Dial E. J., Moore J. E. Naproxen-PC: A GI safe and highly effective anti-inflammatory. Inflammopharmacology 2009; 17, 1–5.
27. Liles J. H., Flecknell P. A. The use of non-steroidal anti-inflammatory drugs for the relief of pain in laboratory rodents and rabbits. Laboratory. Animals. 1992; 26, 241–255.
28. Gola Shefali., Malhotra Anand S., Gupta Asheesh. RP-HPLC assay of ibuprofen in plasma using different extraction procedures. Int. J. of. Bio. Res. 2011; 2, 353–358.
29. Wang X. L., Han J., Zhang D., Liu H. C. Pharmacokinetics of ibuprofen enantiomers in rats after intravenous and oral administration of ibuprofen arginate. Yao. Xue. Xue. Bao. 2012; 47, 88−93.
30. Canapro R., Muntoni E., Zara G. P., Della Pepa C., Berno E., Costa M., Eandi M. Determination of Ibuprofen in human plasma by high-performance liquid chromatography: validation and application in pharmacokinetic study. Biomed. Chromatogr. 2000; 14, 219–226.
31. Minkler P. E., Hoppel C. L. Determination of ibuprofen in human plasma by high-performance liquid chromatography. J. Chromatogr. 1988; 428, 388–394.
32. Ting Li, Liang Fang, Changshun Ren, Manli Wang, Ligang Zhao. Determination of transdermally and orally applied indomethacin in rat plasma and excised skin and muscle samples. AJPS. 2008; 3, 269–275.
33. Bachhav Y. G., Patravale V. B. SMEDDS of glyburide: formulation, in vitro evaluation, and stability studies. AAPS. PharmSciTech. 2009; 10, 482–487.
34. Patel A. R., Vavia P. R. Preparation and in vivo evaluation of SMEDDS (self-microemulsifying drug delivery system) containing fenofibrate. AAPS J. 2007; 9, E344–E352.
35. Pouton C. W. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and self-microemulsifying drug delivery systems. Eur. J. Pharm. Sci. 2000; 11, S93–108.
36. Pouton C. W., Porter C. J. H. Formulation of lipid-based delivery systems for oral administration: materials, methods and strategies. Adv. Drug. Deliv. Rev. 2008; 60, 625–637.
37. Pouton C. W. Formulation of poorly water-soluble drugs for oral administration: physicochemical and physiological issues and the lipid formulation classification system. Eur. J. Pharm. Sci. 2006; 29, 278–287.
38. Osborne D. W., Middleton C. A., Rogers R. L. Alcohol-Free Microemulsions. J. Dispers. Sci. Technol. 1988, 415–423.
39. Groves M. J., Mustafa R. M. Measurement of the spontaneity of self emulsifiable oils. J. Pharm. Pharmcol. 1974; 26, 671–681.
40. Pouton C. W. Self-emulsifying drug delivery systems: assessment of the efficiency of emulsification. Int. J. Pharm. 1985; 27, 335–348.
41. Zhong-gao, Han-Gon Choi, Hee-Jong Shin, Kyung-Mi Park, Soo-Jeong Lim, Ki-Jun Hwang, Chong-Kook Kim. Physicochemical characterization and evaluation of a microemulsion system for oral delivery of cyclosporin A. Int. J. Pharm. 1998; 161, 75–86.
42. Zhang P., Liu Y., Feng N., Xu J. Preparation and evaluation of self-emulsifying drug delivery system of oridonin. Int. J. Pharm. 2008; 355, 269–276.
43. Roland I., Piel G., Delattre L., Evrard B. Systematic characterization of oil- in- water emulsions for formulation design. Int. J. Pharm. 2003; 263, 85–94.
44. Ashish Deshmukh., Shirishkumar Kulkarni. Novel self micro-emulsifying drug delivery systems (SMEDDS) of efavirenz. J. Chem. Pharma. Res. 2012; 4, 3914–3919.
Labels
Pharmacy Clinical pharmacologyArticle was published in
Czech and Slovak Pharmacy
2017 Issue 1
Most read in this issue
- Osudy židovských farmaceutů z českých zemí během holocaustu
- Zdravotnické a nezdravotnické náklady na léčbu a péči Parkinsonovy choroby – srovnání Evropy, USA, Asie a Austrálie
- Samoemulgující systém (SEDDS) pro podání léčiva ibuprofen: hodnocení vzorků v podmínkách in vitro a in vivo
- Cytotoxické, protirakovinné a antimikrobiální účinky extraktů z Artemisia rupestris