Temperature-responsive Expansion of Self-crosslinked Ufasomes of Conjugated Linoleic Acid†

doi:10.7503/cjcu20150079

Abstract

Abstract:

Self-crosslinked ufasomes of conjugated linoleic acid(SCLA ufasomes) were obtained from CLA ufasomes through intravesicular polymerization initiated by mild UV irradiation. Temperature-responsive size and morphology evolutions of the SCLA ufasomes were traced by dynamic light scattering(DLS) and cryo-transmission electron microscope(cryo-TEM), and it was found that not only the vesicular structure of the SCLA ufasomes was stable but also the vesicular volume was expansive hugely with increasing temperature. In vitro release of 5-Fluorouracil(5-FU) from the SCLA ufasomes was evaluated and the results demonstrated that the drug-loading SCLA ufasomes possessed temperature-responsive sustained and controlled release of 5-FU.

Key words: Ufasome, Self-crosslinked conjugated linoleic acid, Morphology, Temperature responsive expansion, In vitro release

CLC Number:

O648

TrendMD:

DAI Jining, FAN Ye, FANG Yun. Temperature-responsive Expansion of Self-crosslinked Ufasomes of Conjugated Linoleic Acid^†[J]. Chem. J. Chinese Universities, 2015, 36(6): 1140.

Figures/Tables 6

Fig.1 Effect of UV-irradiation time on UV spectra of SCLA ufasomespH=8.6; c=3 mmol/L. UV-irradiation time/h: a. 0; b. 0.25; c. 0.5; d. 1; e. 1.5; f. 2; g. 2.5.

Fig.2 Size distribution and morphology of CLA ufasomes and SCLA ufasomes(3 mmol/L, pH=8.6, 25 ℃) (A) Size(2Rh) distribution. a. CLA vesicle, b. self-crosslinked CLA ufasomes with 47% crosslinking degree; (B) cryo-TEM image of CLA ufasomes; (C) cryo-TEM image; (D) TEM image of SCLA ufasomes with 47% polymerization degree.

Fig.3 Size sensitive(A) and structure stable(B) of SCLA ufasomes(3 mmol/L, pH=8.6) at different temperatures (A) Rh/nm: a. 8.1; b. 9.2; c. 10.4; d. 12.1; e. 15.5; f. 16.4. (B) Temperature/℃: a. 25; b. 30; c. 35; d. 40; e. 45; f. 50.

Fig.4 Temperature-responsive expansion of SCLA ufasomes(3 mmol/L, pH=8.6) (A1—A3) Rh distribution; (B1—B3) cryo-TEM images; (C1—C3) assessment of wall thickness. (A1—C1) 25 ℃; (A2—C2) 37 ℃; (A3—C3) 50 ℃.

Fig.5 Release behavior of 5-FU in PBS buffer(A) Standard UV curve; (B) in vitro release curve. a. Free drug, 25 ℃;b. loaded drug, 42 ℃; c. loaded drug, 37 ℃; d. loaded drug, 25 ℃.

Table 1 Formations of in vitro release of 5-FU in PBS buffer

Release temperature/℃	R²				Weibull equation
Release temperature/℃	Zero-order		First-order	Higuchi	Weibull
25^*	0.9056	0.9569	0.9646	0.9892	ln[-ln(1-Q)]=1.24lnt-3.74
25	0.6709	0.8941	0.8093	0.9472	ln[-ln(1-Q)]=0.6401lnt-2.388
37	0.6478	0.8363	0.7951	0.9557	ln[-ln(1-Q)]=0.4877lnt-1.705
42	0.6852	0.9458	0.7549	0.9859	ln[-ln(1-Q)]=0.5748lnt-1.8426

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