Fabrication of Lamellar Liquid Crystals of Conjugated Linoleic Acid as Drug Delivery Systems †

doi:10.7503/cjcu20190682

Abstract

Abstract:

The lamellar liquid crystals in aqueous phase using conjugated linoleic acid(CLA) and its conjugate base sodium conjugated linoleate(SCL) were fabricated, and drug release behavior of the resulted lamellar liquid crystals was investigated. The lamellar liquid crystal phase in the CLA/SCL/H₂O ternary phase diagram was determined by means of polarizing microscopy assisted by visual inspection. The polarized texture, phase parameters and rheological parameters of the lamellar liquid crystals were obtained by polarizing microscope, small-angle X-ray scattering system and rotational rheometer, and the experimental results confirm that the lamellar liquid crystals are suitable for drug delivery system(DDS). The releasing curves of a hydrophilic drug 5-fluorouracil and a lipophilic drug curcumin were measured by dialysis experiments using the drug-loaded lamellar liquid crystals as DDS, and good sustained release abilities for both drugs were provided by the lamellar liquid crystals.

Key words: Conjugated linoleic acid, Lamellar liquid crystal, Rheology, Drug delivery system

CLC Number:

O648

TrendMD:

FAN Ye, LI Qian, FANG Yun, XIA Yongmei. Fabrication of Lamellar Liquid Crystals of Conjugated Linoleic Acid as Drug Delivery Systems ^†[J]. Chem. J. Chinese Universities, 2020, 41(4): 750.

Figures/Tables 9

Fig.1 Phase diagram of CLA/SCL/H2O system at 25 ℃(A), textures of the lamellar liquid crystals(Lα) obtained by polarizing microscopy before(B) and after(C) ultracentrifugation

Fig.2 SAXS patterns of Lα at 25 ℃ corresponding to different water contents(a1—a3)(A) and CLA contents(b1—b3)(B)

Sample	m(CLA)∶m(SCL)∶m(H₂O)	q₁/nm^-1	q₂/nm^-1	d/nm	Phase
a₁	0.25∶0.75∶0.60	1.338		4.65	Lamellar
a₂	0.25∶0.75∶0.70	1.283	2.528	4.89	Lamellar
a₃	0.25∶0.75∶0.80	1.190	2.373	5.28	Lamellar
b₁	0.20∶0.50∶0.50	1.394	2.736	4.51	Lamellar
b₂	0.30∶0.50∶0.50	1.263	2.482	4.98	Lamellar
b₃	0.40∶0.50∶0.50	1.250	2.484	5.03	Lamellar

Fig.3 Viscosity(η) vs. shear rate(γ˙) of the a series(A) and the b series(B) at 25 ℃

Fig.4 Linear viscoelastic region and critical stress of Lα at 25 ℃(A) Stress sweep of a1 at 1 Hz; (B) complex modulus(G*) vs. shear stress(σ) of the a series; (C) stress sweep of b1 at 1 Hz; (D) complex modulus(G*) vs. shear stress(σ) of the b series.

Sample	η^a/(Pa·s)	σ_c/Pa	G'^b/Pa	G″^c/Pa
a₁	2319	235	7691	714
a₂	2052	195	6061	583
a₃	1780	167	4777	369
b₁	934	178	2543	275
b₂	769	85	2672	217
b₃	617	58	1631	168

Fig.5 Storage modulus(G') and loss modulus(G″) as a function of ω for the a series(A) and the b series(B) at 25 ℃

Fig.6 Effect of temperatures on steady-state and dynamic rheology(A) η vs. γ˙of a1; (B) G' and G″ as a function of ω for a1; (C) η vs. γ˙of b1; (D) G' and G″ as a function of ω for b1.

Fig.7 Cumulative release(CR) rate of 5-FU(A) and curcumin(B) in PBS solution at 37 ℃ and schematic illustration for drug release mechanism of lamellar liquid crystal DDS(C)

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