Preparation of Micro/Nano-fibers Membranes Encapsulated with Dual Drugs by Emulsion Electrospun and Controlled Release of Hydrophilic and Hydrophobic Drugs†

doi:10.7503/cjcu20170491

Abstract

Abstract:

Polylactic acid(PLA) and hydrophobic drug of camptothecin(CPT) solution play as the oil(O) phase. At the same time, gelation solution with hydrophilic drug of astragalus polysccharide(APS) play as the water(W) phase. Oil-in-water(O/W) emulsion was prepped by phase reversion method which was the method of low energy. The viscosity of O/W emulsion was adjusted by controlling the concentration and molecular weight of polyethlene glycol(PEG). The PLA/PEG micro/nano-fibers membrane was obtained by emulsion electrospun. On the one hand, the emulsion was characterized by particle size, optical microscope(OM). On the other hand, the scanning electromicroscope(SEM), infrared spectroscopy(FTIR) and X-ray diffraction(XRD) were used to characterize the structure and ingredient of the PLA/PEG micro/nano-fibers membrane. Besides, the hydrophilia and cytotoxicity test were used to evaluate the biocompatibility of PLA/PEG micro/nano-fibers membrane. In order to observe the distribution of drugs, the laser scanning confocal microscopy(CLSM) was used. The results show that different micro-nano structure of PLA/PEG micro/nano-fibers can be successful spinning by emulsion electrospun. Even though different morphology of composite membrane had different hydrophilia, but its hydrophilia was good. At the same time, PLA/PEG micro/nano-fibers membrane had a good biocompatibility with no cytotoxicity. The in vitro release results showed that the accumulative release of drugs in the phosphate buffer solution of pH=5.8 was higher than in the phosphate buffer solution of pH=6.8 and pH=7.4 so that the phosphate buffer solution of pH=5.8 was more advantageous to the release of drugs. As well as we can conclude that APS release faster than CPT. The PLA/PEG micro/nano-fibers membrane can realize differential release of drugs in phosphate buffer solution of pH=5.8.

Key words: Emulsion electrospun, Phase reversion, Polylactic acid/polyethylene glycol micro/nano-fiber, Differential release

CLC Number:

O631.2

TrendMD:

GAO Yan, ZHANG Hua, ZHANG Wen, LI Xiangpeng, YUE Pan, LI Wei. Preparation of Micro/Nano-fibers Membranes Encapsulated with Dual Drugs by Emulsion Electrospun and Controlled Release of Hydrophilic and Hydrophobic Drugs^†[J]. Chem. J. Chinese Universities, 2018, 39(3): 575.

Figures/Tables 11

Scheme 1 Preparation process of drug-load PLA/PEG micro/nano-finer membrane

Fig.1 Diameter distribution of emulsion with different amounts of emulsifierMass fraction of SMA(%): (A)15; (B)20; (C)25.

Fig.2 Optical microscope images of emulsion with different amounts of emulsifierMassfraction of SMA(%): (A)15; (B)20; (C)25.

Fig.3 SEM images of PLA/PEG micro/nano-fiber membrane with different mass fraction and molecular weight of PEGMass fraction and molecular weight of PEG: (A) 30%, Mn= 4000; (B) 15%, Mn=6000; (C) 30%—50%, Mn=8000;(D) 50%, Mn=10000. Insets: contact angle/(°): (A)67.4; (B) 56.8; (C)47.2; (D)35.3.

Fig.4 FTIR spectra of PLA(a), PLA/PEG micro/nano-fiber membrane(P2, b), CPT(c), drug-load PLA/PEG micro/nano-fiber membrane(D2, d), PEG(e) and APS(f)

Fig.5 XRD patterns of PEG(a), drug-load PLA/PEG micro/nano-fibermembrane(P2, b), PLA/PEG micro/nano-fiber membrane(D2, c), CPT(d), PLA(e) and APS(f)

Fig.6 Cell relative proliferation with different morphologies of PLA/PEG micro/nano-fiber membrane in vitroThe cell relative proliferation determined by MTT.

Fig.7 Optical microscope images of cell relative proliferation of PLA/PEG micro/nano-fiber membrane(P3) in vitro in difference culture timeTime/h: (A) 24; (B) 48; (C) 72. (D) Blank control.

Fig.8 CLSM images of cell proliferation in vitro with PLA/PEG micro/nano-fiber membrane(P2) Time/h: (A) 24; (B) 48; (C) 72.

Fig.9 Hydrophilic drug distribution in different morphologies of PLA/PEG micro/nano-fiber membrane(A) String-in-beads, 20%SMA, 30%PEG(Mn=8000), 5%DOX; (B) nano-fibers, 20%SMA, 50%PEG(Mn=10000), 5%DOX.

Fig.10 Cumulative release of APS(a—c) and CPT(a'—c') from different morphologies of PLA/PEG micro/nano-fiber membrane in the buffer solution of various pH(A) pH=5.8; (B) pH=6.8; (C) pH=7.4. a', c. Discrete beads morphology(D1);b, b'. string-in-beads morphology(D2); a, c'. nano fibers morphology(D3).

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