Exemestane encapsulated copolymers L121/F127/GL44 based mixed micelles: solubility enhancement and in vitro cytotoxicity evaluation using MCF-7 breast cancer cells

Singh, Gurdeep; Singh, Davinder; Choudhari, Manisha; Kaur, Simran; Dubey, Sunil Kumar; Arora, Saroj; Bedi, Neena

doi:10.1007/s40005-021-00540-0

Cited by 16 publications

(7 citation statements)

References 37 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Among the tested carriers, povidone K30 (PVP K30) and poloxamer 407 (P407) enhanced indirubin solubility the most, by about 15–18 fold compared to pure MT-102 ( Figure 2 ). This result may be explained by better wettability, reduced particle size, and a change in drug crystallinity [ 8 , 26 ]. In general, adding a surfactant to an SD formulation should lower the degree of supersaturation, preventing nucleation and thermodynamic crystal growth, and thus inhibiting drug precipitation while improving drug dissolution [ 27 ].…”

Section: Resultsmentioning

confidence: 99%

“…Therefore, the solubilization of MT-102 is critical to improving its therapeutic potential and clinical application. Prodrugs, salt formation, micronization, solid dispersion, and lipid-based formulations have all been developed to improve the oral bioavailability of poorly soluble drugs [ 7 , 8 , 9 ]. Among them, solid dispersion (SD) is an effective method for increasing the solubility and dissolution of hydrophobic herbal products [ 10 ].…”

Section: Introductionmentioning

confidence: 99%

See 1 more Smart Citation

Enhanced Oral Bioavailability of MT-102, a New Anti-inflammatory Agent, via a Ternary Solid Dispersion Formulation

et al. 2022

View full text Add to dashboard Cite

This study aimed to develop a solid dispersion (SD) of MT-102, a new anti-inflammatory agent, to improve its oral bioavailability. The ternary SD formulations of MT-102 (a poorly soluble extract of Isatis indigotica and Juglans mandshurica) were prepared using a solvent evaporation method with various drug/excipient ratios. Following that, the effectiveness of various SDs as an oral formulation of MT-102 was investigated using indirubin as a marker component. By forming SDs with hydrophilic polymers, the aqueous solubility of indirubin was significantly increased. SD-F4, containing drug, poloxamer 407 (P407), and povidone K30 (PVP K30) at a 1:2:2 weight ratio, exhibited the optimal dissolution profiles in the acidic to neutral pH range. Compared to pure MT-102 and a physical mixture, SD-F4 increased indirubin’s dissolution from MT-102 by approximately 9.86-fold and 2.21-fold, respectively. Additionally, SD-F4 caused the sticky extract to solidify, resulting in improved flowability and handling. As a result, compared to pure MT-102, the oral administration of SD-F4 significantly improved the systemic exposure of MT-102 in rats. Overall, the ternary SD formulation of MT-102 with a blended mixture of P407 and PVP K30 appeared to be effective at improving the dissolution and oral absorption of MT-102.

show abstract

Section: Resultsmentioning

confidence: 99%

Section: Introductionmentioning

confidence: 99%

Enhanced Oral Bioavailability of MT-102, a New Anti-inflammatory Agent, via a Ternary Solid Dispersion Formulation

et al. 2022

View full text Add to dashboard Cite

show abstract

“…The HLB value of the surfactant is an important variable for selecting the proper surfactant. The surfactants are either w/o type (HLB of [3][4][5][6][7][8] or o/w type (HLB of 8-16). In w/o emulsions, low HLB value surfactants i.e., less than 8 are utilized.…”

Section: Surfactant Systemmentioning

confidence: 99%

“…Various techniques have been employed to increase the solubility of active moieties. These techniques include physical and chemical modification of API along with formulation strategies, which include particle size reduction, complexation, amorphization, and nano-carrier drug delivery systems as represented in Figure 1 [ 2 , 3 , 4 ].…”

Section: Introductionmentioning

confidence: 99%

Nanoemulgel: A Novel Nano Carrier as a Tool for Topical Drug Delivery

et al. 2023

Self Cite

View full text Add to dashboard Cite

Nano-emulgel is an emerging drug delivery system intended to enhance the therapeutic profile of lipophilic drugs. Lipophilic formulations have a variety of limitations, which includes poor solubility, unpredictable absorption, and low oral bioavailability. Nano-emulgel, an amalgamated preparation of different systems aims to deal with these limitations. The novel system prepared by the incorporation of nano-emulsion into gel improves stability and enables drug delivery for both immediate and controlled release. The focus on nano-emulgel has also increased due to its ability to achieve targeted delivery, ease of application, absence of gastrointestinal degradation or the first pass metabolism, and safety profile. This review focuses on the formulation components of nano-emulgel for topical drug delivery, pharmacokinetics and safety profiles.

show abstract

“…DLS data was generated at 25°C with a fixed 90° light incidence angle. All measurements were replicated of three experiments ( Singh et al, 2021b ).…”

Section: Introductionmentioning

confidence: 99%

Development and optimization of nanoparticles loaded with erucin, a dietary isothiocyanate isolated from Eruca sativa: Antioxidant and antiproliferative activities in ehrlich-ascites carcinoma cell line

Singh

Attri

et al. 2023

Front. Pharmacol.

Self Cite

View full text Add to dashboard Cite

The study on Erucin (ER) has gained interest of nutraceutical and pharmaceutical industries because of its anti-cancer properties. Erucin is an isothiocyanate obtained from the seeds of Eruca sativa which possess certain drawbacks such as poor aqueous solubility and bioavailability. Therefore, the present study aimed at developing ER-cubosomes (CUB) by solvent evaporation technique followed by applying Central Composite Design to optimize ER loaded cubosomes. For this purpose, independent variables selected were Monoolein (MO) as lipid and Pluronic-84 (P-84) as a stabilizer whereas dependent variables were particle size, percentage of ER loading and percentage of its entrapment efficiency. The cubosomal nanocarriers exhibited particle size in the range of 26 nm, entrapment efficiency of 99.12 ± 0.04% and drug loading of 3.96 ± 0.0001%. Furthermore, to investigate the antioxidant potential, we checked the effect of ER and ER-CUB by DNA nicking assay, DDPH assay and Phosphomolybdate assay, and results showed significant improvement in antioxidant potential for ER-CUB than ER. Similarly, ER-CUB showed enhanced anticancer activity with a marked reduction in IC50 value than ER in MTT assay. These results suggested that ER-CUB produced notable escalation in antioxidant potential and enhanced anticancer activity than ER.

show abstract

Exemestane encapsulated copolymers L121/F127/GL44 based mixed micelles: solubility enhancement and in vitro cytotoxicity evaluation using MCF-7 breast cancer cells

Cited by 16 publications

References 37 publications

Enhanced Oral Bioavailability of MT-102, a New Anti-inflammatory Agent, via a Ternary Solid Dispersion Formulation

Enhanced Oral Bioavailability of MT-102, a New Anti-inflammatory Agent, via a Ternary Solid Dispersion Formulation

Nanoemulgel: A Novel Nano Carrier as a Tool for Topical Drug Delivery

Development and optimization of nanoparticles loaded with erucin, a dietary isothiocyanate isolated from Eruca sativa: Antioxidant and antiproliferative activities in ehrlich-ascites carcinoma cell line

Contact Info

Product

Resources

About