Polymeric micelles loaded with glyburide and vanillic acid: I. Formulation development, in-vitro characterization and bioavailability studies

Kaur, Jaskiran; Gulati, Monica; Famta, Paras; Corrie, Leander; Awasthi, Ankit; Saini, Sumant; Khatik, Gopal L.; Bettada, Vidya G.; Madhunapantula, SubbaRao V.; Paudel, Keshav Raj; Gupta, Gaurav; Chellappan, Dinesh Kumar; Arshad, Mohammed Faiz; Adams, Jon; Kuppusamy, Gowthamarajan; Dua, Kamal; Hansbro, Philip M.; Singh, Sachin Kumar

doi:10.1016/j.ijpharm.2022.121987

Cited by 24 publications

(6 citation statements)

References 35 publications

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“…The relative bioavailability was found to be 4791% for XH loaded in SLNs, and the relative bioavailability of naive XH was 20.80%. This indicated about 230.33-folds enhancement in bioavailability upon loading XH into SLN as compared to naive XH [61,63,64]. Hence, the results of the release studies were found in concordance with pharmacokinetic studies.…”

Section: In Vivo Pharmacokinetic Studysupporting

confidence: 71%

“…Further, the results revealed about 1.07-fold enhancement in Cmax upon loading XH into SLNs as its value was 20,730 ng/mL for XH that got enhanced to 22,350 ng/mL. This indicated higher absorption of XH loaded in SLNs [61,63]. Similarly, the results of AUC0-t revealed about 4.7-fold enhancement in its result for XH upon loading into SLNs as that of naive XH (Table 7, Figure 11).…”

Section: In Vivo Pharmacokinetic Studymentioning

confidence: 85%

“…The lipases present in the GIT break the triglycerides into the surface-active mono-and diacylglycerols that further stimulate the secretion of bile salt endogenously [65][66][67]. Overall, it may help in enhancing oral bioavailability [62,63].…”

Section: In Vivo Pharmacokinetic Studymentioning

confidence: 99%

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Quality by Design Based Formulation of Xanthohumol Loaded Solid Lipid Nanoparticles with Improved Bioavailability and Anticancer Effect against PC-3 Cells

et al. 2022

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Many natural products with greater therapeutic efficacy are limited to target several chronic diseases such as cancer, diabetes, and neurodegenerative diseases. Among the natural products from hops, i.e., Xanthohumol (XH), is a prenylated chalcone. The present research work focuses on the enhancement of the poor oral bioavailability and weak pharmacokinetic profile of XH. We exemplified the development of a Xanthohumol-loaded solid lipid nanoparticles (XH-SLNs) cargo system to overcome the limitations associated with its bioavailability. The XH-SLNs were prepared by a high-shear homogenization/ultrasonication method and graphical, numerical optimization was performed by using Box–Behnken Design. Optimized XH-SLNs showed PS (108.60 nm), PDI (0.22), ZP (−12.70 mV), %EE (80.20%) and an amorphous nature that was confirmed by DSC and PXRD. FE-SEM and HRTEM revealed the spherical morphology of XH-SLNs. The results of release studies were found to be 9.40% in 12 h for naive XH, whereas only 28.42% of XH was released from XH-SLNs. The slow release of drugs may be due to immobilization of XH in the lipid matrix. In vivo pharmacokinetic study was performed for the developed XH-SLNs to verify the enhancement in the bioavailability of XH than naive XH. The enhancement in the bioavailability of the XH was confirmed from an increase in Cmax (1.07-folds), AUC0-t (4.70-folds), t1/2 (6.47-folds) and MRT (6.13-folds) after loading into SLNs. The relative bioavailability of XH loaded in SLNs and naive XH was found to be 4791% and 20.80%, respectively. The cytotoxicity study of naive XH, XH-SLNs were performed using PC-3 cell lines by taking camptothecin as positive control. The results of cytotoxicity study revealed that XH-SLNs showed good cell inhibition in a sustained pattern. This work successfully demonstrated formulation of XH-SLNs with sustained release profile and improved oral bioavailability of XH with good anticancer properties against PC-3 cells.

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Section: In Vivo Pharmacokinetic Studysupporting

confidence: 71%

Section: In Vivo Pharmacokinetic Studymentioning

confidence: 85%

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Quality by Design Based Formulation of Xanthohumol Loaded Solid Lipid Nanoparticles with Improved Bioavailability and Anticancer Effect against PC-3 Cells

et al. 2022

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“…Detergent properties and emulsifying capacity of cations are quite weakand they are quite expensive. In the previous studies, CTAB is not used alone to enhance solubility/bioavailability but also give cationic charge/sterical stabilization [58,59]. In CTAB-based solid dispersion formulations, the water solubility capacity was increased from 0.802±0.174 to 226.899±6.595, 432.595±6.022, 589.768±0.559 µg/mL, respectively.…”

Section: Preparation Of Solid Dispersionsmentioning

confidence: 99%

Solubilization Effect of Anionic, Cationic and Nonionic Surfactants on Coenzyme Q10 Solid Dispersion

ERGİN¹

2023

jrp

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Coenzyme Q10 ( CoQ10) is an oil-soluble vitamin-like benzoquinone compound. Coenzyme Q10 plays a role in providing membrane stability, energy conversion and ATP production. It is also one of the important antioxidants in the body. The bioavailability of coenzyme Q10 is very low due to its low solubility in water and its large molecular mass. Among the solubility enhancement approaches, solid dispersions (SDs) are one of the most promising strategies. The use of suitable carrier and methodology plays a significant role in the biological response. In terms of a carrier, solid dispersions are classified broadly the third group. Surfactant-based SDs are called third-generation solid dispersions. To evaluate the surfactant effect on solubilization of CoQ10, three different surfactants of varying ratios between 1:1, 1:3 and 1:5 (w/w) were used namely sodium dodecylsulfate (SDS) (anionic), cetyl trimethyl ammonium bromide (CTAB) (cationic) and Pluronic F127 (non-ionic). CoQ10 solid dispersions were characterized in terms of particle size, polydispersity index, zeta potential, FTIR spectroscopy, DSC analysis, saturation solubility and in vitro dissolution studies. To compare dissolution rate, area under the dissolution curve (AUC), Mean Dissolution Time (MDT), mean residence time of the drug substance molecules in the dosage form (MRT), and dissolutio nefficiency % (DE%) were calculated. All the formulations showed improvement in the aqueous solubility, while the dissolution rate was increased only by Pluronic F127 (p<0.05). Among the surfactants, Pluronic F127-based SDs were found superior to other surfactants. The results revealed that surfactant-based SDs offered great success in improving the therapeutic efficacy of CoQ10.

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“…However, VA has poor solubility which leads to its poor bioavailability, of about 25% [7], as it is well known for its dissolution rate-limited bioavailability [8]. Thus, the formulation of VA into nanocarriers could help in the enhancement of its bioavailability.…”

Section: Introductionmentioning

confidence: 99%

Response surface optimization of a cardioprotective compound through pharmacosomal drug delivery system: in vivo bioavailability and cardioprotective activity potential

Dawoud

Zaafan

Saleh

et al. 2023

Drug Deliv. and Transl. Res.

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Vanillic acid (VA) is a phenolic compound with potential antioxidant activity, which improves ischemia-induced myocardial degeneration, by reducing oxidative stress; however, it suffers poor bioavailability owing to its poor solubility. VA-loaded pharmacosomes were optimized using a central composite design, where the effect of phosphatidylcholine:VA molar ratio and the precursor concentration were studied. An optimized formulation (O1) was prepared and tested for the release rate of VA, in vivo bioavailability, and cardioprotective potential on myocardial infarction-induced rats. The optimized formulation showed a particle size of 229.7 nm, polydispersity index of 0.29, and zeta potential of − 30 mV. O1 showed a sustained drug release for 48 h. The HPLC–UV method was developed for the determination of VA in plasma samples using protein precipitation. The optimized formulation showed a great improvement in the bioavailability as compared to VA. The residence time of the optimized formula was 3 times longer than VA. The optimized formulation showed a more potent cardioprotective effect as compared to VA, via inhibition of the MAPK pathway with subsequent inhibition of PI3k/NF-κB signaling, in addition to its antioxidant effect. The optimized formulation showed normalization of many oxidative stress and inflammatory biomarkers. Thus, a VA-loaded pharmacosome formulation with promising bioavailability and cardioprotective activity potential was prepared. Graphical Abstract

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Polymeric micelles loaded with glyburide and vanillic acid: I. Formulation development, in-vitro characterization and bioavailability studies

Cited by 24 publications

References 35 publications

Quality by Design Based Formulation of Xanthohumol Loaded Solid Lipid Nanoparticles with Improved Bioavailability and Anticancer Effect against PC-3 Cells

Quality by Design Based Formulation of Xanthohumol Loaded Solid Lipid Nanoparticles with Improved Bioavailability and Anticancer Effect against PC-3 Cells

Solubilization Effect of Anionic, Cationic and Nonionic Surfactants on Coenzyme Q10 Solid Dispersion

Response surface optimization of a cardioprotective compound through pharmacosomal drug delivery system: in vivo bioavailability and cardioprotective activity potential

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