Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

Rarokar, Nilesh R.; Saoji, Suprit D.; Raut, Nishikant A.; Taksande, Jayashree B.; Khedekar, Pramod B.; Dave, Vivek S

doi:10.1208/s12249-015-0369-y

Cited by 91 publications

(41 citation statements)

References 49 publications

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“…The zeta potential of the prepared CN was found to be −35.0±1.9 mV. These results are in agreement with previous reports, which mentions that the zeta potential values of greater than −30 mV are considered acceptable, and are indicative of a good physical stability (42,43).…”

Section: Particle Size and Zeta Potential Analysissupporting

confidence: 92%

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Saoji

Raut

Dhore

et al. 2015

AAPS J

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Abstract. In the present study, a phospholipid-based complex of standardized Centella extract (SCE) was developed with a goal of improving the bioavailability of its phytoconstituents. The SCE-phospholipid complex was prepared by solvent evaporation method and characterized for its physicochemical and functional properties. Fourier transform infrared spectroscopy (FTIR), differential scanning calorimetry (DSC), scanning electron microscopy (SEM), photomicroscopy, and powder x-ray diffraction (PXRD) were used to confirm the formation of Centella naturosome (CN). The prepared complex was functionally evaluated by apparent solubility, in vitro drug release, ex vivo permeation, and in vivo efficacy studies. The prepared CN exhibited a significantly higher (12-fold) aqueous solubility (98.0±1.4 μg/mL), compared to the pure SCE (8.12±0.44 μg/mL), or the physical mixture of SCE and the phospholipid (13.6±0.4 μg/mL). The in vitro dissolution studies revealed a significantly higher efficiency of CN in releasing the SCE (99.2±4.7, % w/w) in comparison to the pure SCE (39.2±2.3, % w/w), or the physical mixture (42.8±2.09, % w/w). The ex vivo permeation studies with the everted intestine method showed that the prepared CN significantly improved the permeation of SCE (82.8±3.7, % w/w), compared to the pure SCE (26.8±2.4, % w/w), or the physical mixture (33.0±2.7, % w/w). The in vivo efficacy studies using the Morris Water Maze test indicated a significant improvement of the spatial learning and memory in aged mice treated with CN. Thus, drug-phospholipid complexation appears to be a promising strategy to improve the aqueous solubility and bioavailability of bioactive phytoconstituents.

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Section: Particle Size and Zeta Potential Analysissupporting

confidence: 92%

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Saoji

Raut

Dhore

et al. 2015

AAPS J

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“…Cubosome structure consists of a highly twisted, continuous lipid bilayer with two congruent, non-intersecting water channels [19]. Compared to the simple bilayer structure of liposomes, cubosomes have increased surface area and strong ability to encapsulate diverse molecules from hydrophilic, hydrophobic, and amphiphilic substances [20]. The cubosomes possess higher physiochemical stability than liposomes due to the strong electric repulsion and a large ratio of lipid bilayer [21][22][23].…”

Section: Introductionmentioning

confidence: 99%

Ocular Cubosome Drug Delivery System for Timolol Maleate: Preparation, Characterization, Cytotoxicity, Ex Vivo, and In Vivo Evaluation

Huang

Peng

et al. 2017

AAPS PharmSciTech

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Glaucoma is an ocular disease featuring increased intraocular pressure (IOP) and its primary treatment strategy is to lower IOP by medication. Current ocular drug delivery in treating glaucoma is confronting a variety of challenges, such as low corneal permeability and bioavailability due to the unique anatomical structure of the human eye. To tackle these challenges, a cubosome drug delivery system for glaucoma treatment was constructed for timolol maleate (TM) in this study. The TM cubosomes (liquid crystalline nanoparticles) were prepared using glycerol monooleate and poloxamer 407 via high-pressure homogenization. These constructed nanoparticles appeared spherical using transmission electron microscopy and had an average particle size of 142 nm, zeta potential of -6.27 mV, and over 85% encapsulation efficiency. Moreover, using polarized light microscopy and small-angle X-ray scattering (SAXS), it was shown that the TM cubosomes have cubic liquid crystalline D-type (Pn3m) structure, which provides good physicochemical stability and high encapsulation efficiency. Ex vivo corneal permeability experiments showed that the total amount of TM cubosomes penetrated was higher than the commercially available eye drops. In addition, in vivo studies revealed that TM cubosomes reduced the IOP in rabbits from 27.8∼39.7 to 21.4∼32.6 mmHg after 1-week administration and had a longer retention time and better lower-IOP effect than the commercial TM eye drops. Furthermore, neither cytotoxicity nor histological impairment in the rabbit corneas was observed. This study suggests that cubosomes are capable of increasing the corneal permeability and bioavailability of TM and have great potential for ocular disease treatment.

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“…In the next step the diglyceride undergoes the same process and 2-monoglyceride is produced. Both hydrolysis [22] and alcoholysis [35,36] have been described for preparation of 2-monoglycerides.…”

Section: Alcoholysismentioning

confidence: 99%

Progress in Synthesis of Monoglycerides for Use in Food and Pharmaceuticals

et al. 2017

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Glycerides are lipid esters of the glycerol molecule and fatty acids. Their primary function is the storage of energy. Due to its structure and properties, glycerol participates in the formulation or synthesis of many compounds such as food products, cosmetics, pharmaceuticals, liquid detergents. Monoglycerides (MGs) can be formed by both industrial chemical glycerolysis and biological or enzymatic processes. Chemical glycerolysis bring issues of low MGs yield, high operating temperature, formation of undesirable by-products and high energy consumption. On the other hand enzymatic processes have advantages of mild reaction conditions and high purity of MGs. But, several purification steps are required to obtain food or pharmaceutical grade MG, such as neutralization of the reaction media and discoloration followed by expensive molecular distillation. The purpose of this article is to review the main challenges in the synthesis of MGs from triglycerides (TGs) contained in the various fixed oils and application thereof in the food and pharmaceuticals.

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Nanostructured Cubosomes in a Thermoresponsive Depot System: An Alternative Approach for the Controlled Delivery of Docetaxel

Cited by 91 publications

References 49 publications

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Preparation and Evaluation of Phospholipid-Based Complex of Standardized Centella Extract (SCE) for the Enhanced Delivery of Phytoconstituents

Ocular Cubosome Drug Delivery System for Timolol Maleate: Preparation, Characterization, Cytotoxicity, Ex Vivo, and In Vivo Evaluation

Progress in Synthesis of Monoglycerides for Use in Food and Pharmaceuticals

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