Zwanden Sule YAHAYA, Danjuma MALLAM, Rukayyat Bukola OLOYEDE, Olutayo Ademola ADELEYE, Gideon Owoicho OKPANACHI, Fatima Shuaibu KURFI

Preliminary research on ibuprofen self-emulsifying formulation

Ibuprofen is an important and commonly used nonsteroidal anti-inflammatory medication (NSAID). Its medicinal potentials are however severely hindered due to its poor water solubility and low oral absorption. A selfnano emulsifying drug delivery system (SNEDDS) is a lipid formulation that takes advantage of the solubilizing capacity of a mixture of oil, surfactant, and cosurfactant to improve intestinal permeability. The aim of this study is to develop SNEDDS of ibuprofen employing both labrafac CC and a natural lipophile (N-L) (vegetable oil) from pressed sesame seeds to improve the anti-inflammatory activity of ibuprofen. The formulation was stable against phase separation and drug precipitation, exhibited rapid emulsification within 5 s to yield an emulsion with a mean droplet size of 27.23 nm and showed a significant (p = 0.000) increase in anti-inflammatory properties compare to the aqueous suspension of the standard drug and each treatment agent across the test period. Overall, SNEDDS of ibuprofen with desirable physicochemical properties and improved anti-inflammatory activities were successfully developed using an un-refined lipophile obtained from pressed sesame seed.

PDF

___

[1] Williams HD, Trevaskis NL, Charman SA, Shanker RM, Charman WN, Pouton CW, Porter CJH. Strategies to address low drug solubility in discovery and development. Pharmacol Rev 2013; 65(1): 315-499. [CrossRef]
[2] Yahaya ZS, Ofokansi KC, Allagh ST, Bhatia PG. Preparation and characterization of artemether inclusion complexes with hydroxypropyl-β-cyclodextrin. Trop J Pharm Res. 2017; 16(10): 2359-2364. [CrossRef]
[3] Boyd BJ, Bergström CAS, Vinarov Z, Kuentz M, Brouwers J, Augustijns P, Brandl M, Bernkop-Schnürch A, Shresta N, Préat V, Müllertz A, Bauer-Brandl A, Jannin V. Successful oral delivery of poorly water-soluble drugs both depends on the intraluminal behavior of drugs and of appropriate advanced drug delivery systems. Eur J Pharm Sci. 2019; 137:104967. [CrossRef]
[4] Yahaya ZS, Yahaya PO, Mohammed BB. Preliminary investigation on coconut oil-based self-emulsifying formulation for the delivery of metronidazole. Nig J Pharm Appl Sci Res. 2020; 9(1):18-24.
[5] Yahaya ZS, Oyi AR, Allagh TS, Abdulsamad A. Solid self-emulsifying drug delivery system for artemether with improved physicochemical properties: design and characterization. West Afr J Pharm. 2020; 31(1) 164 - 175.
[6] Atef E, Belmonte AA. Formulation and in vitro and in vivo characterization of a phenytoin self-emulsifying drug delivery system (SEDDS). Eur J Pharm Sci. 2008; 35(4): 257–263. [CrossRef]
[7] Kassem AA, Mohsen AM, Ahmed RS, Essam TM. Self-nanoemulsifying drug delivery system (SNEDDS) with enhanced solubilization of nystatin for treatment of oral candidiasis: design, optimization, in vitro and in vivo evaluation. J Mol Liq. 2016; 218(1): 219–232. [CrossRef]
[8] Tripathi CB, Beg S, Kaur R, Shukla G, Bandopadhyay S, Singh B. Systematic development of optimized SNEDDS of artemether with improved biopharmaceutical and antimalarial potential. Drug Deliv. 2016; 23(9): 3209–3223. [CrossRef]
[9] Mandawgade SD, Sharma S, Pathak S, Patravale VB. Development of SMEDDS using natural lipophile: Application to β-artemether delivery. Int J Pharm. 2008; 362(1-2):179–183. [CrossRef]
[10] Obitte CA. Preliminary attempt to address indomethacins poor water solubility using solid self-emulsifying drug delivery system as a carrier. Afr J Pharm Pharmacol. 2013; 7(49): 2918–2927. [CrossRef]
[11] Potthast H, Dressman JB, Junginger HE, Midha KK, Oeser H, Shah VP, Vogelpoel H, Barends DM. Biowaiver monographs for immediate release solid oral dosage forms: Ibuprofen. J Pharm Sci. 2005; 94(10): 2121–2131. [CrossRef]
[12] Neslihan Gursoy R, Benita S. Self-emulsifying drug delivery systems (SEDDS) for improved oral delivery of lipophilic drugs. Biomed Pharmacother. 2004; 58(3): 173–182. [CrossRef]
[13] Obitte NC, Rohan LC, Adeyeye CM, Esimone CO. Optimized artemether-loaded anhydrous emulsion. Br J Pharm Res. 2014; 4(1): 37–59.
[14] Yahaya Z, Oyi A, Allagh T, Abdulsamad A. Development and characterization of self-nano emulsifying drug delivery system of ibuprofen. J Pharm Res Int. 2018; 23(2): 1–13. [CrossRef]
[15] Zhang P, Liu Y, Feng N, Xu J. Preparation and evaluation of self-micro emulsifying drug delivery system of oridonin. Int J Pharm. 2008; 355(1-2):269–276. [CrossRef]
[16] Feeney OM, Crum MF, McEvoy CL, Trevaskis NL, Williams HD, Pouton CW, Charman WN, Bergström CAS, Poerter CHJ. 50 years of oral lipid-based formulations: Provenance, progress and future perspectives. Adv Drug Deliv Rev. 2016; 101:167–194. [CrossRef]
[17] Olorunsola EO. Self-Emulsifying Drug Delivery System. Pharmaceutics in Focus: Dosage Form Development And Manufacture. 1st ed., Zaria, Nigeria: Ahmadu Bello University Press Ltd; 2021, p. 377–89.
[18] Yahaya ZS, Oyi AR, Allagh TS, Abdulsamad A. Piroxicam-loaded self-emulsifying drug delivery system. Nig J Pharm 2019; 53(1): 34-47.
[19] Obitte NC, Ugorji L, Ezichi L, Ogbodo S, Onyishi V, Chukwu A. Ibuprofen self-emulsifying drug delivery system. World J Pharm Pharm Sci. 2015; 4(2): 887–889.
[20] Obitte NC, Ofokansi KC, Kenechukwu FC. Development and evaluation of novel self-nanoemulsifying drug delivery systems based on a homolipid from Capra hircus and its admixtures with melon oil for the delivery of indomethacin. J Pharm (Cairo). 2014; 2014: 340486 [CrossRef]
[21] Winter CA, Risley EA, Nuss GW. Anti-inflammatory and antipyretic activities of indomethacin. J Pharmacol Exp Ther. 1963; 141:367–376.
[22] Okoli CO. Analgesic and anti-inflammatory agents. A handbook of techniques in experimental pharmacology. 1st ed., Benin, Nigeria: Mindex Publishing company Ltd; 2019, p. 171–81.