Abstract
A large proportion of new chemical moieties are poorly water-soluble. As a result, the biggest challenge for researchers is to enhance the solubility and oral bioavailability of lipophilic drugs. Self-emulsifying systems offer immense potential for improving lipophilic drugs’ oral bioavailability and solubility through various mechanisms such as: inhibiting efflux transporters, absorption of the lipophilic drug through the lymphatic system, and bypassing hepatic first-pass metabolism. These systems dissolve hydrophobic drugs, allowing them to be delivered in a unit dose form for oral administration. Despite much potential, issues like stability, low drug loading, packaging, etc., are associated with the self-emulsifying technique. This review discusses conventional Self-Emulsifying Drug Delivery Systems (SEDDS), which deliver poorly water-soluble drugs. Recent advancements in self-emulsifying systems to solve the issues associated with conventional SEDDS are described exhaustively, including their methodologies and excipients utilized for preparation. The current article also furnishes a literature review on recent advancements in self-emulsifying systems. Recent advances in SEDDS are a great option for overcoming oral bioavailability, stability, and solubility issues of lipophilic drugs. Solid-self emulsifying system can be used to improve the stability of the formulation, hydrophobic ion-pairing for improving mucus permeation properties, while supersaturated self-emulsifying systems with a low concentration of surfactant to overcome issues such as precipitation of drug after dilution and gastrointestinal related side effects. The day will come when medicine companies will see the value of selfemulsifying system developments and adopt this technology for next-generation product releases.
Keywords: Eutectic, hydrophobic ion pairing, lipophilic drugs, osmotic, phospholipid complex, self double emulsifying drug delivery systems, self emulsifying drug delivery systems
Graphical Abstract
[http://dx.doi.org/10.1208/s12249-018-1212-z] [PMID: 30617712]
[http://dx.doi.org/10.1016/j.jaim.2017.02.007] [PMID: 29229368]
[http://dx.doi.org/10.1080/21691401.2019.1581791] [PMID: 30888204]
[http://dx.doi.org/10.5530/jyp.2017.9.68]
[http://dx.doi.org/10.1016/j.jddst.2018.06.014]
[http://dx.doi.org/10.1208/s12249-019-1421-0] [PMID: 31187334]
[http://dx.doi.org/10.1016/j.molliq.2016.02.081]
[http://dx.doi.org/10.1208/s12249-016-0632-x] [PMID: 27677262]
[http://dx.doi.org/10.1016/j.apsb.2017.02.002] [PMID: 28540173]
[http://dx.doi.org/10.2147/IJN.S190426] [PMID: 30863054]
[http://dx.doi.org/10.1007/s40005-016-0279-3]
[http://dx.doi.org/10.1016/j.ejpb.2009.03.001] [PMID: 19298857]
[http://dx.doi.org/10.1007/s40005-016-0243-2]
[http://dx.doi.org/10.1016/j.ijpharm.2018.11.010] [PMID: 30408530]
[http://dx.doi.org/10.1208/s12249-017-0857-3] [PMID: 28975598]
[http://dx.doi.org/10.1080/10837450.2017.1335321] [PMID: 28540754]
[http://dx.doi.org/10.1016/j.arabjc.2021.103321]
[http://dx.doi.org/10.3390/nano11112858] [PMID: 34835622]
[http://dx.doi.org/10.1016/j.ijpharm.2020.119180] [PMID: 32135227]
[http://dx.doi.org/10.3390/pharmaceutics14020336] [PMID: 35214068]
[http://dx.doi.org/10.1080/10717544.2017.1344335] [PMID: 28675315]
[http://dx.doi.org/10.3109/10717544.2014.885615] [PMID: 24524289]
[http://dx.doi.org/10.1016/j.jddst.2017.01.002]
[http://dx.doi.org/10.1016/j.ijpharm.2018.02.020] [PMID: 29458210]
[http://dx.doi.org/10.3109/03639045.2014.886695] [PMID: 24517575]
[http://dx.doi.org/10.3109/03639045.2014.938655] [PMID: 25019500]
[http://dx.doi.org/10.1016/j.bfopcu.2017.02.001]
[http://dx.doi.org/10.1080/07373937.2016.1201833]
[http://dx.doi.org/10.1016/j.jconrel.2021.08.013] [PMID: 34384795]
[http://dx.doi.org/10.1016/j.ijpharm.2017.05.036] [PMID: 28528850]
[http://dx.doi.org/10.1016/j.xphs.2017.01.001] [PMID: 28087316]
[http://dx.doi.org/10.1016/j.jcis.2020.11.051] [PMID: 33234314]
[http://dx.doi.org/10.1016/j.drudis.2008.04.006] [PMID: 18598917]
[PMID: 24511474]
[http://dx.doi.org/10.1007/s40005-017-0344-6]
[http://dx.doi.org/10.1016/j.jpha.2018.01.004] [PMID: 29922487]
[http://dx.doi.org/10.3109/03639045.2014.900081] [PMID: 24641324]
[http://dx.doi.org/10.1016/j.ejps.2016.08.050] [PMID: 27590128]
[http://dx.doi.org/10.4103/0975-1483.51868]
[http://dx.doi.org/10.1208/s12249-017-0743-z] [PMID: 28236269]
[http://dx.doi.org/10.3109/03639045.2015.1058816] [PMID: 26177197]
[http://dx.doi.org/10.1016/j.ejps.2019.06.007] [PMID: 31175944]
[http://dx.doi.org/10.1007/s40005-016-0263-y]
[http://dx.doi.org/10.1007/s40005-015-0225-9]
[http://dx.doi.org/10.1208/s12248-015-9832-7] [PMID: 26486790]
[http://dx.doi.org/10.1016/j.ajps.2018.11.009] [PMID: 32636951]
[http://dx.doi.org/10.2147/IJN.S136599] [PMID: 28507434]
[http://dx.doi.org/10.3390/pharmaceutics11020058] [PMID: 30708963]
[http://dx.doi.org/10.2147/IJN.S149717] [PMID: 29263669]
[http://dx.doi.org/10.3390/polym9040124] [PMID: 30970802]
[PMID: 27051286]
[http://dx.doi.org/10.3109/21691401.2014.966192] [PMID: 25331709]
[http://dx.doi.org/10.1007/s12272-013-0202-7] [PMID: 23852645]
[http://dx.doi.org/10.1016/j.ijpharm.2013.10.044] [PMID: 24184217]
[http://dx.doi.org/10.1002/jps.21451] [PMID: 18543293]
[http://dx.doi.org/10.1016/j.colsurfa.2011.12.025]
[http://dx.doi.org/10.26452/ijrps.v11i2.2242]
[http://dx.doi.org/10.1016/j.apsb.2018.09.004] [PMID: 30766782]
[http://dx.doi.org/10.1016/j.ijpharm.2013.05.014] [PMID: 23688622]
[http://dx.doi.org/10.1208/s12249-017-0936-5] [PMID: 29340982]
[http://dx.doi.org/10.4103/2045-080X.112809]
[http://dx.doi.org/10.1080/03639040601150328] [PMID: 17891586]
[http://dx.doi.org/10.5402/2012/528079] [PMID: 22852100]
[http://dx.doi.org/10.1016/j.ijpharm.2009.11.026] [PMID: 19961910]
[http://dx.doi.org/10.1166/jbn.2012.1371] [PMID: 22515097]
[http://dx.doi.org/10.2147/IJN.S108765] [PMID: 27713630]
[http://dx.doi.org/10.1016/j.ajps.2018.10.003] [PMID: 32104482]
[http://dx.doi.org/10.1016/j.apsb.2014.03.002] [PMID: 26579386]
[http://dx.doi.org/10.15171/apb.2017.005] [PMID: 28507935]
[http://dx.doi.org/10.1016/j.jsps.2014.11.001] [PMID: 26106276]
[PMID: 22267925]
[http://dx.doi.org/10.3109/03639045.2010.495752] [PMID: 21073324]
[http://dx.doi.org/10.1113/jphysiol.1972.sp010027] [PMID: 4646578]
[http://dx.doi.org/10.3109/09687688009063882] [PMID: 7432184]
[http://dx.doi.org/10.1208/s12249-019-1319-x] [PMID: 30790136]
[http://dx.doi.org/10.1039/C5RA11687B]
[http://dx.doi.org/10.1016/j.jddst.2016.04.011]
[http://dx.doi.org/10.1016/j.ijpharm.2015.07.048] [PMID: 26211900]
[http://dx.doi.org/10.3109/10717544.2016.1143056] [PMID: 26923905]
[http://dx.doi.org/10.1016/j.jconrel.2018.03.018] [PMID: 29574041]
[http://dx.doi.org/10.1016/j.ijpharm.2014.05.047] [PMID: 24879935]
[http://dx.doi.org/10.1016/j.jconrel.2018.01.012] [PMID: 29355620]
[http://dx.doi.org/10.1080/03639045.2017.1338722] [PMID: 28589736]
[http://dx.doi.org/10.1016/j.ejpb.2016.09.013] [PMID: 27693677]
[http://dx.doi.org/10.1016/j.jcis.2018.07.057] [PMID: 30036849]
[http://dx.doi.org/10.1016/j.ijpharm.2011.02.047] [PMID: 21356300]
[http://dx.doi.org/10.1016/j.colsurfa.2015.11.017]
[http://dx.doi.org/10.1002/ejlt.201600167]
[PMID: 22888246]
[http://dx.doi.org/10.1166/nmb.2014.1011]
[http://dx.doi.org/10.1016/j.jddst.2017.06.014]
[http://dx.doi.org/10.1177/0885328215617891] [PMID: 26637442]
[http://dx.doi.org/10.1039/C7FO00439G] [PMID: 28640295]
[http://dx.doi.org/10.1208/s12249-010-9568-8] [PMID: 21181511]
[http://dx.doi.org/10.1208/s12249-012-9912-2] [PMID: 23319299]
[http://dx.doi.org/10.1016/S0378-5173(02)00003-0] [PMID: 11879759]
[http://dx.doi.org/10.1016/j.ijpharm.2018.02.019] [PMID: 29458206]
[http://dx.doi.org/10.1016/j.ejpb.2016.11.019] [PMID: 27876599]
[http://dx.doi.org/10.1080/10717544.2016.1214990] [PMID: 27685505]