Improved dissolution of oleanolic acid with ternary solid dispersions

Liu, Longxiao; Wang, Xiaocui

doi:10.1208/pt0804113

Cited by 43 publications

(25 citation statements)

References 27 publications

(21 reference statements)

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“…The original powder shows an endothermic/exothermic transition (T t = 251.6-260 ºC, H t = 77.33 kJ/mol) and a second endotherm (T f = 304 ºC, H f = 78.23 kJ/mol). The endothermic peak found for PVP K30 between T g =150-190°C is due to glass transition temperature and also on the moisture content, this result was also reported by other workers [13,14]. MB may exist under three polymorphic forms, A, B and C and the thermal events found correspond to the most stable and less soluble polymorph A.…”

Section: Solid Phase Characterizationsupporting

confidence: 85%

“…The lack of a melting peak in the DSC of a solid dispersion indicates that the drug is present in an amorphous rather than a crystalline form, i.e., exist conversions of crystalline form to partial amorphous state. This is due to the amorphous form of MB in the solid dispersion, possibly because the carrier acts inhibiting crystallization [14].…”

Section: Solid Phase Characterizationmentioning

confidence: 99%

See 1 more Smart Citation

Physicochemical Characterization and Solubility Enhancement Studies of Mebendazole Solid Dispersions in Solvent Mixtures

Ángeles¹,

Escalera²,

Pena-Fernandez³

et al. 2016

JPP

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Abstract:The objective was to obtain solid dispersion to improve the dissolution rate, solubility and oral absorption of MB (mebendazole), poor water-soluble drugs. The new formulation was characterized by DSC (differential scanning calorimetry), PXRD (powder X-ray diffraction), FT-IR (fourier transform infrared spectroscopy) and STEM (scanning transmission electron microscopy) methods. Solid dispersions of MB with polyvinylpyrrolidone K-30 (PVP K30) were prepared by solvent evaporation method. The solubility of MB (original powder) and that of the solid dispersions was measured at 25ºC in ethanol-water. The aqueous solubility of MB was favoured by the presence of the polymer in solvent mixtures. Combination of solid dispersions with co-solvents increased the water solubility of MB in a larger extent that each method separately. Solubility parameter () was used to relate to solubility profiles. MB and the solid dispersions show a solubility curve with a single peak at ı = 30.78 MPa 1/2 . Solid state characterizations indicated that the solid dispersion exist an amorphous material entrapped in polymer matrix getting highest improvement in wettability and solubility.

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Section: Solid Phase Characterizationsupporting

confidence: 85%

Section: Solid Phase Characterizationmentioning

confidence: 99%

Physicochemical Characterization and Solubility Enhancement Studies of Mebendazole Solid Dispersions in Solvent Mixtures

Ángeles¹,

Escalera²,

Pena-Fernandez³

et al. 2016

JPP

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show abstract

“…During the testing, it was noted that the SRSD sinks immediately, whereas the pure drug kept floating on the surface for a longer time interval. These results indicated a CA-enhanced wettability of Cur and a carrier-controlled dissolution in the SRSD (19). The content of mannitol also affected drug dissolution from SRSD.…”

Section: Dissolution Testingmentioning

confidence: 74%

Improved Bioavailability of Poorly Water-Soluble Drug Curcumin in Cellulose Acetate Solid Dispersion

et al. 2011

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Abstract. Curcumin (Cur), one of the most widely used natural active constituents with a great variety of beneficial biological and pharmacological activities, is a practically water-insoluble substance with a short biologic half-life. The aim of this study was to develop a sustained-release solid dispersion by employing water-insoluble carrier cellulose acetate for solubility enhancement, release control, and oral bioavailability improvement of Cur. Solid dispersions were characterized by solubility, in vitro drug release, Fourier transform infrared spectroscopy, X-ray diffractometry, and differential scanning calorimetry studies. The in vivo performance was assessed by a pharmacokinetic study. Solid-state characterization techniques revealed the amorphous nature of Cur in solid dispersions. Solubility/ dissolution of Cur was enhanced in the formulations in comparison with pure drug. Sustained-release profiles of Cur from the solid dispersions were ideally controlled in vitro up to 12 h. The optimized formulation provided an improved pharmacokinetic parameter (C max =187.03 ng/ml, t max =1.95 h) in rats as compared with pure drug (C max =87.06 ng/ml, t max =0.66 h). The information from this study suggests that the developed solid dispersions successfully enhanced the solubility and sustained release of poorly water-soluble drug Cur, thus improving its oral bioavailability effectively.

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“…Some dosage forms of OA have been introduced such as liposomes, 15 nanoliposomes, 16 nanoparticle suspension, 17 oral microemulsion, 18 and solid dispersions, 19 but they showed some shortcomings, such as poor long-term stability, small drug loading, and unobvious release effect. Multivesicular liposomes (MVLs) have received great attention due to their excellent stability and longer duration of release.…”

Section: Introductionmentioning

confidence: 99%

Effect of a controlled-release drug delivery system made of oleanolic acid formulated into multivesicular liposomes on hepatocellular carcinoma in vitro and in vivo

Luo¹,

Liu²,

Zhang³

et al. 2016

IJN

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The aim of the present study was to develop a novel dosage form of multivesicular liposomes for oleanolic acid (OA) to overcome its poor solubility, prolong therapeutic drug levels in the blood, and enhance the antitumor effect on hepatocellular carcinoma. OA-encapsulated multivesicular liposomes (OA-MVLs) were prepared by a double-emulsion method, and the formulation was optimized by the central composite design. The morphology, particle size, and drug-loading efficiency of OA-MVLs were investigated. Furthermore, OA-MVLs were also characterized both in vitro and in vivo. The results showed that OA-MVLs were spherical particles with an average particle size of 11.57 μm and an encapsulation efficiency of 82.3%±0.61%. OA-MVLs exhibited a sustained-release pattern in vitro, which was fitted to Ritger–Peppas equation. OA-MVLs inhibited the growth of human HepG2 cells which was confirmed by the MTT assay and fluorescence microscopy detection. The in vivo release of OA from OA-MVLs exhibited a sustained manner, indicating a longer circulation time compared to OA solution. The in vivo toxicity study indicated that medium-dose OA-MVLs exerted no toxic effect on the hosts. Importantly, OA-MVLs suppressed the growth of murine H22 hepatoma and prolonged the survival of tumor-bearing mice. In conclusion, the poorly soluble OA could be encapsulated into MVLs to form a novel controlled-release drug delivery system. The present study may hold promise for OA-MVLs as a new dosage form for sustained-release drug delivery in cancer therapy.

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Improved dissolution of oleanolic acid with ternary solid dispersions

Cited by 43 publications

References 27 publications

Physicochemical Characterization and Solubility Enhancement Studies of Mebendazole Solid Dispersions in Solvent Mixtures

Physicochemical Characterization and Solubility Enhancement Studies of Mebendazole Solid Dispersions in Solvent Mixtures

Improved Bioavailability of Poorly Water-Soluble Drug Curcumin in Cellulose Acetate Solid Dispersion

Effect of a controlled-release drug delivery system made of oleanolic acid formulated into multivesicular liposomes on hepatocellular carcinoma in vitro and in vivo

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