Mixed micelles loaded with silybin-polyene phosphatidylcholine complex improve drug solubility

Duan, Rui-ling; Sun, Xun; Liu, Jie; Gong, Tao; Zhang, Zhirong

doi:10.1038/aps.2010.192

Cited by 50 publications

(38 citation statements)

References 33 publications

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“…Thus, the optimized mass ratio of PC to SDC got from the experiment basically accorded with the above discussion. The micro-morphology showed that the CUR-PC-SDC-MMs prepared through thin film dispersed method were spherical, which is consistent with the previous report (Duan et al, 2011). In terms of the aggregate structure, lots of researchers have studied on bile salt/PC mixed micelles by a series of methods such as static and dynamic light scattering, small-angle neutron scattering, small angle x-ray scattering and cryo-TEM (Long et al, 1994).…”

Section: Discussionsupporting

confidence: 85%

“…High DL% and EE% maybe ascribed to the potential mechanization that PC and SDC reveal the strongest bonding force (Duan et al, 2011) when the mass ratio is at 0.264. The aggregation system of PCs alone is liquid crystalline bilayer structure instead of micelle, which is difficult to be digested (Tang et al, 2009).…”

Section: Discussionmentioning

confidence: 99%

“…For organism, bile salts, secreted by liver and stored in the gall bladder, could form a kind of stable mixed micellar system with PCs, glycerides and fatty acids during lipid digestion in the small intestine Duan et al, 2011). The bile salt/PC micelles can package cholesterol inside the hydrophobic core, and the solubility, stability and bioavailability of poorly water-soluble drugs could be enhanced in the same way (Dangi et al, 1995;Garidel et al, 2007).…”

Section: Introductionmentioning

confidence: 99%

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Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

et al. 2014

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Although curcumin (CUR) can inhibit proliferation and induce apoptosis of tumors, the poor water solubility restricted its clinical application. The aim of this study was to improve the aqueous solubility of CUR and make more favorable changes to bioactivity by preparing curcumin-loaded phospholipid-sodium deoxycholate-mixed micelles (CUR-PC-SDC-MMs). CUR-PC-SDC-MMs were prepared by the thin-film dispersion method. Based on the results of single factor exploration, the preparation technology was optimized using the central composite design-response surface methodology with drug loading and entrapment efficiency (EE%) as indicators. The images of transmission electron microscopy showed that the optimized CUR-PC-SDC-MMs were spherical and well dispersed. The average size of the mixed micelles was 66.5 nm, the zeta potential was about À26.96 mV and critical micelle concentration was 0.0087 g/l. CUR was encapsulated in PC-SDC-MMs with loading capacity of 13.12%, EE% of 87.58%, and the solubility of CUR in water was 3.14 mg/ml. The release results in vitro showed that the mixed micelles presented sustained release behavior compared to the propylene glycol solution of CUR. The IC 50 values of CUR-loaded micelles and free drug in human breast carcinoma cell lines were 4.10 mg/ml and 6.93 mg/ml, respectively. It could be concluded from the above results that the CUR-PC-SDC-MMs system might serve as a promising nanocarrier to improve the solubility and bioactivity of CUR.

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Section: Discussionsupporting

confidence: 85%

Section: Discussionmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

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Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

et al. 2014

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“…A number of alternative technologies are being developed to overcome the drawbacks associated with poor aqueous solubility, for example, including use of surfactants [3], micronization [4], inclusion complexation [5] and solid dispersion [6]. Among these solid dispersion has gained importance as a promising approach, as the other methods suffer from limitation like size reduction by micronization, results in the formation of surface charge on particles which restrict their flow and exhibit poor flow properties [7].…”

Section: Introductionmentioning

confidence: 99%

Improvement in Dissolution of Bosentan Monohydrate by Solid Dispersions Using Spray Drying Technique

Dangre¹,

Sormare²,

Godbole³

2017

PHARMSCI

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Background:Bosentan monohydrate (BM), a dual endothelin receptor antagonist, is indicated for the treatment of patients with pulmonary arterial hypertension (PAH). It is poorly soluble in water, and having absolute bioavailability of 50%. Objective:The aim of the present work is to develop and evaluate the solid dispersions (SD) of a poorly water soluble drug bosentan monohydrate (BM). Method:Solid dispersions (SDs) systems of BM were prepared with Hydroxy propyle β-cyclodextrin (HPβ-CD) and Polyethylene glycol (PEG-4000) polymers using a spray drying technique. Result:The significant rise in a saturation solubility 174.23±1.36 mg/mL; and drug dissolution 95.11±1.22%; was observed with optimized formulation (SD 6). The solid state characterization of optimized formulation (SD 6) by SEM, DSC, and XRPD revealed the absence of crystalline nature of BM in solid dispersion. High dissolution rate of solid dispersion (SD 6) compared with pure drug indicated the increase in dissolution characteristics. Conclusion:In conclusion, our studies illustrated that spray drying technique could be useful large scale producing method to prepare the solid dispersion of bosentan with HP β-CD, which can improve the solubility as well as stability of the formulation.

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“…19 Due to their good physiological compatibility and excellent solubilizing capacity, bile salt micelles and derived mixed systems have been intensively investigated as drug-carrier systems. [20][21][22] Previous investigations into bile salt/phospholipid MMs has mainly focused on the solubilization of insoluble drugs, 18,[23][24][25] structural identification, 26 physicochemical properties, 27 and transmembrane characteristics; 17 however, bile salt/ phospholipid MMs may also be good candidates for oral delivery of poorly water-soluble drugs.…”

Section: Introductionmentioning

confidence: 99%

Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating

Dong¹,

Xie²,

Qi³

et al. 2013

IJN

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Bile salt/phospholipid mixed micelles (MMs) are potent carriers used for oral absorption of drugs that are poorly soluble in water; however, there are many limitations associated with liquid formulations. In the current study, the feasibility of preparing bile salt/ phospholipid MM precursor (preMM) pellets with high oral bioavailability, using fluid-bed coating technology, was examined. In this study, fenofibrate (FB) and sodium deoxycholate (SDC) were used as the model drug and the bile salt, respectively. To prepare the MMs and to serve as the micellular carrier, a weight ratio of 4:6 was selected for the sodium deoxycholate/ phospholipids based on the ternary phase diagram. Polyethylene glycol (PEG) 6000 was selected as the dispersion matrix for precipitation of the MMs onto pellets, since it can enhance the solubilizing ability of the MMs. Coating of the MMs onto the pellets using the fluid-bed coating technology was efficient and the pellets were spherical and intact. MMs could be easily reconstituted from preMM pellets in water. Although they existed in a crystalline state in the preMM pellets, FB could be encapsulated into the reconstituted MMs, and the MMs were redispersed better than solid dispersion pellets (FB:PEG = 1:3) and Lipanthyl ® . The redispersibility of the preMM pellets increased with the increase of the FB/PEG/micellar carrier. PreMM pellets with a FB:PEG:micellar carrier ratio of 1:1.5:1.5 showed 284% and 145% bioavailability relative to Lipanthyl ® and solid dispersion pellets (FB:PEG = 1:3), respectively. Fluid-bed coating technology has considerable potential for use in preparing sodium deoxycholate/phospholipid preMM pellets, with enhanced oral bioavailability for poorly water-soluble drugs.

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Mixed micelles loaded with silybin-polyene phosphatidylcholine complex improve drug solubility

Cited by 50 publications

References 33 publications

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

Curcumin-loaded mixed micelles: preparation, optimization, physicochemical properties and cytotoxicityin vitro

Improvement in Dissolution of Bosentan Monohydrate by Solid Dispersions Using Spray Drying Technique

Bile salt/phospholipid mixed micelle precursor pellets prepared by fluid-bed coating

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