Pegylated Oleic Acid-Lecithin Liposomes (Poll) for Anticancer Drug Delivery

Abstract

Cancer is a major health issue, conferring to more than 14.5 million deaths worldwide. Liposomes, self-assembly amphiphilic bilayer molecules, served as excellent alternative vehicles due to their ability to encapsulate both hydrophobic and hydrophilic anticancer drugs. Conventional liposomes, comprised mainly phospholipids are costineffective, unstable, and easily degraded by the external environment. In this study, we introduced PEGylated oleic acid-lecithin liposomes constructed by using C-18 monounsaturated fatty acids (oleic acid) and soy lecithin, in the presence of DOPEPEG2000 in pH7.4, above their glass transition temperature, T g , by employing the simple thin layer lipid hydration method. FTIR spectrum of oleic acid, soy lecithin, and DOPEPEG2000 was studied. The average particle size without further mechanical interference was 1102.3 nm while the zeta potential value was -18 mV, which is compatible with the zeta potential of the red blood cell. The polydispersity index (PDI) was reduced by 46.2% with the incorporation of the DOPEPEG2000. The morphological study using OPM showed the presence of spherical shape liposomes that exhibit the birefringence effect under the light field and Maltese cross under the dark field. Encapsulation of folinic acid, methotrexate, doxorubicin, or irinotecan resulted in greater than 75% encapsulation efficiency (EE). Half-maximal inhibitory concentration, IC 50 , was significantly reduced in POLL as compared to free anticancer drugs. Our data demonstrate POLL may be a promising alternative vehicle to deliver various anticancer drugs to targeted tumour sites. ABSTRAKBarah merupakan isu kesihatan utama yang menyebabkan lebih 14.5 juta kematian di seluruh dunia. Liposom, iaitu molekul swabentuk dwilapis merupakan penghantar alternatif terbaik berikutan kebolehannya untuk mengkapsulkan ubatan anti barah hidrofobik dan hidrofilik. Liposom yang lazimnya diperbuat daripada fosfolipid adalah tidak efektif daripada segi kos, tidak stabil dan mudah terurai oleh persekitaran luar. Dalam kajian ini, kami memperkenalkan liposom asid olik-lesitin berPEG yang terdiri daripada asid lemak tak tepu C-18 (asid olik) dan lesitin soya, dengan kehadiran DOPEPEG2000 dalam pH7.4, pada suhu lebih tinggi daripada suhu peralihan gelas T g , menggunakan metod hidrasi lapisan nipis lipid. Spektrum FTIR asid olik, lesitin soya, dan DOPEPEG2000 juga turut dikaji. Purata saiz partikel adalah 1102.3 nm manakala keupayaan zeta adalah -18 mV, sesuai dengan keupayaan zeta sel darah merah. Indeks polisebaran telah berkurang sebanyak 46.2% dengan penambahan DOPEPEG2000. Kajian morfologi menggunakan Mikroskop Optikal Pengutuban menunjukkan kewujudan liposom berbentuk sfera yang menghasilkan kesan dwibiasan pada medan cerah dan silang Maltese pada medan gelap. Pengkapsulan asid folinik, metotreksat, doksorubisin atau irinotecan menghasilkan lebih 75% kecekapan pengkapsulan. Kepekatan separa rencatan, IC 50 , telah berkurang dengan signifikan pada POLL berbanding ubatan anti barah. Data menunjukkan POLL mungkin ...