Development of Solid Self-Emulsifying Formulation for Improving the Oral Bioavailability of Erlotinib

AAPS PharmSciTech

Volumn 17, Issue 2, 2016, Pages 466-473

  Truong, Duy Hieu ^a   Tran, Tuan Hiep ^a   Ramasamy, Thiruganesh ^a   Choi, Ju Yeon ^a   Lee, Hee Hyun ^a   Moon, Cheol ^b   Choi, Han Gon ^c   Yong, Chul Soon ^a   Kim, Jong Oh ^a  

^a Yeungnam University   (South Korea)

^b Sunchon National University   (South Korea)

^c Hanyang University   (South Korea)

Author keywords

bioavailability; erlotinib; SEDDS; spray drying

Indexed keywords

AEROSIL; COSURFACTANT; DEXTRAN; DEXTRAN 40; DIETHYLENE GLYCOL MONOETHYL ETHER; ERLOTINIB; LABRASOL; SILICON DIOXIDE; ACYLGLYCEROL; EMULSION; EXCIPIENT; POWDER; SURFACTANT;

ANIMAL EXPERIMENT; AREA UNDER THE CURVE; ARTICLE; CONTROLLED STUDY; DIFFERENTIAL SCANNING CALORIMETRY; DRUG BIOAVAILABILITY; DRUG DELIVERY SYSTEM; DRUG FORMULATION; DRUG RELEASE; DRUG SOLUBILITY; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; POWDER X RAY DIFFRACTION; PRIORITY JOURNAL; RAT; SOLID STATE; SPRAY DRYING; X RAY DIFFRACTION; ANIMAL; BIOAVAILABILITY; CHEMISTRY; EMULSION; MEDICINAL CHEMISTRY; ORAL DRUG ADMINISTRATION; PARTICLE SIZE; POWDER; PROCEDURES; SOLUBILITY; SPRAGUE DAWLEY RAT;

ADMINISTRATION, ORAL; ANIMALS; AREA UNDER CURVE; BIOLOGICAL AVAILABILITY; CHEMISTRY, PHARMACEUTICAL; DEXTRANS; DRUG DELIVERY SYSTEMS; EMULSIONS; ERLOTINIB HYDROCHLORIDE; EXCIPIENTS; GLYCERIDES; PARTICLE SIZE; POWDERS; RATS; RATS, SPRAGUE-DAWLEY; SILICON DIOXIDE; SOLUBILITY; SURFACE-ACTIVE AGENTS; X-RAY DIFFRACTION;

EID: 84938633081     PISSN: None     EISSN: 15309932     Source Type: Journal    
DOI: 10.1208/s12249-015-0370-5     Document Type: Article

References (44)

1. van Erp NP, Gelderblom H, Guchelaar H-J. Clinical pharmacokinetics of tyrosine kinase inhibitors. Cancer Treat Rev. 2009;35(8):692–706.
2. Hidalgo M, Siu LL, Nemunaitis J, Rizzo J, Hammond LA, Takimoto C, et al. Phase I and pharmacologic study of OSI-774, an epidermal growth factor receptor tyrosine kinase inhibitor, in patients with advanced solid malignancies. J Clin Oncol. 2001;19(13):3267–79.
3. Scheffler M, Di Gion P, Doroshyenko O, Wolf J. Clinical pharmacokinetics of tyrosine kinase inhibitors. Clin Pharmacokinet. 2011;50(6):371–403.
4. Tan AR, Yang X, Hewitt SM, Berman A, Lepper ER, Sparreboom A, et al. Evaluation of biologic end points and pharmacokinetics in patients with metastatic breast cancer after treatment with erlotinib, an epidermal growth factor receptor tyrosine kinase inhibitor. J Clin Oncol. 2004;22(15):3080–90.
5. Kommuru T, Gurley B, Khan M, Reddy I. Self-emulsifying drug delivery systems (SEDDS) of coenzyme Q10: formulation development and bioavailability assessment. Int J Pharm. 2001;212(2):233–46.
6. Borhade V, Nair H, Hegde D. Design and evaluation of self-microemulsifying drug delivery system (SMEDDS) of tacrolimus. AAPS PharmSciTech. 2008;9(1):13–21.
7. Kale AA, Patravale VB. Design and evaluation of self-emulsifying drug delivery systems (SEDDS) of nimodipine. AAPS PharmSciTech. 2008;9(1):191–6.
8. Date AA, Nagarsenker M. Design and evaluation of self-nanoemulsifying drug delivery systems (SNEDDS) for cefpodoxime proxetil. Int J Pharm. 2007;329(1–2):166–72.
9. Villar AMS, Naveros BC, Campmany ACC, Trenchs MA, Rocabert CB, Bellowa LH. Design and optimization of self-nanoemulsifying drug delivery systems (SNEDDS) for enhanced dissolution of gemfibrozil. Int J Pharm. 2012;431(1):161–75.
10. Mandawgade SD, Sharma S, Pathak S, Patravale VB. Development of SMEDDS using natural lipophile: application to β-artemether delivery. Int J Pharm. 2008;362(1):179–83.
11. Balakrishnan P, Lee BJ, Oh DH, Kim JO, Lee YI, Kim DD, et al. Enhanced oral bioavailability of coenzyme Q10 by self-emulsifying drug delivery systems. Int J Pharm. 2009;374:66–72.
12. Eman Atef AAB. Formulation and in vitro and in vivo characterization of a phenytoin self-emulsifying drug delivery system (SEDDS). Eur J Pharm Sci. 2008;35:257–63.
13. Dixit AR, Rajput SJ, Patel SG. Preparation and bioavailability assessment of SMEDDS containing valsartan. AAPS Pharmscitech. 2010;11(1):314–21.
14. S-x C, S-f N, Li L, Wang C-g, Pan W-s, J-p S. Preparation and evaluation of self-microemulsifying drug delivery system containing vinpocetine. Drug Dev Ind Pharm. 2009;35(5):603–11.
15. Zhang P, Liu Y, Feng N, Xu J. Preparation and evaluation of self-microemulsifying drug delivery system of oridonin. Int J Pharm. 2008;355(1):269–76.
16. Balakumar K, Raghavan CV, Abdu S. Self nanoemulsifying drug delivery system (SNEDDS) of rosuvastatin calcium: design, formulation, bioavailability and pharmacokinetic evaluation. Colloids Surf B: Biointerfaces. 2013;112:337–43.
17. Gupta S, Chavhan S, Sawant KK. Self-nanoemulsifying drug delivery system for adefovir dipivoxil: design, characterization, in vitro and ex vivo evaluation. Colloids Surf A Physicochem Eng Asp. 2011;392(1):145–55.
18. Elnaggar YS, El-Massik MA, Abdallah OY. Self-nanoemulsifying drug delivery systems of tamoxifen citrate: design and optimization. Int J Pharm. 2009;380(1):133–41.
19. Fahmy UA, Ahmed OA, Hosny KM. Development and evaluation of avanafil self-nanoemulsifying drug delivery system with rapid onset of action and enhanced bioavailability. AAPS PharmSciTech. 2014:1–6
20. Dwivedi P, KHATIK R, Khandelwal K, Srivastava R, TANEJA I, Raju KSR, et al. Self-nanoemulsifying drug delivery system (SNEDDS) for oral delivery of arteether: pharmacokinetics, toxicity and antimalarial activity in mice. RSC Adv. 2014.
21. Tran TH, Guo Y, Song D, Bruno RS, Lu X. Quercetin‐containing self‐nanoemulsifying drug delivery system for improving oral bioavailability. J Pharm Sci. 2014;103(3):840–52.
22. Mahmoud DB, Shukr MH, Bendas ER. In vitro and in vivo evaluation of self-nanoemulsifying drug delivery systems of cilostazol for oral and parenteral administration. Int J Pharm. 2014.
23. Khan AW, Kotta S, Ansari SH, Sharma RK, Ali J. Self-nanoemulsifying drug delivery system (SNEDDS) of the poorly water-soluble grapefruit flavonoid Naringenin: design, characterization, in vitro and in vivo evaluation. Drug Deliv. 2014;(0):1–10.
24. Singh G, Pai RS. Optimized self-nanoemulsifying drug delivery system of atazanavir with enhanced oral bioavailability: in vitro/in vivo characterization. Expert Opin Drug Deliv. 2014;(0):1–10.
25. Bandyopadhyay S, Katare O, Singh B. Optimized self nano-emulsifying systems of ezetimibe with enhanced bioavailability potential using long chain and medium chain triglycerides. Colloids Surf B: Biointerfaces. 2012;100:50–61.
26. Mohd AB, Sanka K, Bandi S, Diwan PV, Shastri N. Solid self-nanoemulsifying drug delivery system (S-SNEDDS) for oral delivery of glimepiride: development and antidiabetic activity in albino rabbits. Drug Deliv. 2014;(0):1–10.
27. Kang JH, Oh DH, Oh Y-K, Yong CS, Choi H-G. Effects of solid carriers on the crystalline properties, dissolution and bioavailability of flurbiprofen in solid self-nanoemulsifying drug delivery system (solid SNEDDS). Eur J Pharm Biopharm. 2012;80(2):289–97.
28. Seo YG, Kim DH, Ramasamy T, Kim JH, Marasini N, Oh Y-K, et al. Development of docetaxel-loaded solid self-nanoemulsifying drug delivery system (SNEDDS) for enhanced chemotherapeutic effect. Int J Pharm. 2013;452(1):412–20.
29. Kim DW, Kang JH, Oh DH, Yong CS, Choi H-G. Development of novel flurbiprofen-loaded solid self-microemulsifying drug delivery system using gelatin as solid carrier. J Microencapsul. 2012;29(4):323–30.
30. Balakrishnan P, Lee B-J, Oh DH, Kim JO, Hong MJ, Jee J-P, et al. Enhanced oral bioavailability of dexibuprofen by a novel solid self-emulsifying drug delivery system (SEDDS). Eur J Pharm Biopharm. 2009;72(3):539–45.
31. Kim GG, Poudel BK, Marasini N, Lee DW, Hiep TT, Yang KY, et al. Enhancement of oral bioavailability of fenofibrate by solid self-microemulsifying drug delivery systems. Drug Dev Ind Pharm. 2013;39(9):1431–8.
32. Sermkaew N, Ketjinda W, Boonme P, Phadoongsombut N, Wiwattanapatapee R. Liquid and solid self-microemulsifying drug delivery systems for improving the oral bioavailability of andrographolide from a crude extract of Andrographis paniculata. Eur J Pharm Sci. 2013;50(3):459–66.
33. Marasini N, Tran TH, Poudel BK, Choi H-G, Yong CS, Kim JO. Statistical modeling, optimization and characterization of spray-dried solid self-microemulsifying drug delivery system using design of experiments. Chem Pharm Bull. 2013;61(2):184–93.
34. Kim DW, Kwon MS, Yousaf AM, Balakrishnan P, Park JH, Kim DS, et al. Comparison of a solid SMEDDS and solid dispersion for enhanced stability and bioavailability of clopidogrel napadisilate. Carbohydrate Polymers. 2014.
35. Oh DH, Kang JH, Kim DW, Lee B-J, Kim JO, Yong CS, et al. Comparison of solid self-microemulsifying drug delivery system (solid SMEDDS) prepared with hydrophilic and hydrophobic solid carrier. Int J Pharm. 2011;420(2):412–8.
36. Prasad Y, Puthli S, Eaimtrakarn S, Ishida M, Yoshikawa Y, Shibata N, et al. Enhanced intestinal absorption of vancomycin with Labrasol and D-α-tocopheryl PEG 1000 succinate in rats. Int J Pharm. 2003;250(1):181–90.
37. Hu Z, Tawa R, Konishi T, Shibata N, Takada K. A novel emulsifier, Labrasol, enhances gastrointestinal absorption of gentamicin. Life Sci. 2001;69(24):2899–910.
38. Rama Prasad Y, Minamimoto T, Yoshikawa Y, Shibata N, Mori S, Matsuura A, et al. In situ intestinal absorption studies on low molecular weight heparin in rats using Labrasol as absorption enhancer. Int J Pharm. 2004;271(1):225–32.
39. Pouton CW. Lipid formulations for oral administration of drugs: non-emulsifying, self-emulsifying and ‘self-microemulsifying’ drug delivery systems. Eur J Pharm Sci. 2000;11:S93–8.
40. Constantinides PP, Scalart J-P, Lancaster C, Marcello J, Marks G, Ellens H, et al. Formulation and intestinal absorption enhancement evaluation of water-in-oil microemulsions incorporating medium-chain glycerides. Pharm Res. 1994;11(10):1385–90.
41. Tarr BD, Yalkowsky SH. Enhanced intestinal absorption of cyclosporine in rats through the reduction of emulsion droplet size. Pharm Res. 1989;6(1):40–3.
42. Parmar N, Singla N, Amin S, Kohli K. Study of cosurfactant effect on nanoemulsifying area and development of lercanidipine loaded (SNEDDS) self nanoemulsifying drug delivery system. Colloids Surf B: Biointerfaces. 2011;86(2):327–38.
43. Muralidhara RD, Parthasaradhi RB, Raji RR, Rathnakar RK, Srinivasa RT. A novel hydrated form of erlotinib free base and a process for preparation of erlotinib hydrochloride polymorph form a substantially free of polymorph form b. Google Patents; 2010.
44. Chudasama A, Shah B, Patel V, Nivsarkar M, Vasu K, Shishoo C. Development of self emulsifying drug delivery system of itraconazole for oral delivery: formulation and pharmacokinetic consideration. J Pharm Investig. 2015;45(3):271–83.