Improved oral bioavailability of the anticancer drug catechin using chitosomes: Design, in-vitro appraisal and in-vivo studies

2019 ◽  
Vol 565 ◽  
pp. 488-498 ◽  
Author(s):  
Hadeer M. Ezzat ◽  
Yosra S.R. Elnaggar ◽  
Ossama Y. Abdallah
Keyword(s):  
Anticancer Drug ◽  
Oral Bioavailability ◽  
In Vivo Studies

scholarly journals ANTICANCER ACTIVITY OF UPAVISHA ARKA: AN OVERVIEW

2020 ◽  
Vol 9 (6) ◽  
pp. 175-181
Author(s):  
Chandekar Deepali Boudhadas ◽  
Pawade Uday Venkatrao ◽  
Nikam Ashwin Vithalrao ◽  
Anjankar Meghsham Pramodrao
Keyword(s):  
Anticancer Activity ◽  
Anticancer Drugs ◽  
Anticancer Drug ◽  
Cost Effective ◽  
In Vivo Studies ◽  
Calotropis Procera ◽  
Calotropis Gigantea ◽  
Natural Derivative

Cancer is one amongst the dreadful diseases of present century. The incidence of cancer is increasing worldwide. Every year about 8,00,000 new cancer patients get registered with the national cancer registry program in India. Ayurveda an ancient Indian medicine science describes many useful herbal drugs for such types of advanced diseases. Upavisha the plant poisons of low potency are mentioned in Agadtantra. Arka (Calotropis procera/ Calotropis gigantea) is one among these Upavisha is emerging as an effective anticancer drug. It shows various pharmacological activities such as Anticancer, Antimicrobial, Antiimplantation etc. Different parts of Arka are used to treat cancer. In current scenario number of synthetic anticancer drugs are used to treat cancer. These synthetic anticancer drugs are expensive and shows harmful adverse effects. Upavisha like Arka which is natural derivative may be cost effective & less harmful as Anticancer drug. Anticancer activity of Calotropis procera/Calotropis gigantea is reported in scientific journals. This review summarizes various In Vitro and In Vivo studies of anticancer activity of Upavisha Arka.

scholarly journals Fabrication of Carbamazepine Cocrystals: Characterization, In Vitro and Comparative In Vivo Evaluation

2021 ◽  
Vol 2021 ◽  
pp. 1-9
Author(s):  
Muhammad Wasim ◽  
Abdul Mannan ◽  
Muhammad Hassham Hassan Bin Asad ◽  
Muhammad Imran Amirzada ◽  
Muhammad Shafique ◽  
...  
Keyword(s):  
Physicochemical Properties ◽  
Oral Bioavailability ◽  
In Vivo Studies ◽  
Aliphatic Chain ◽  
Dissolution Profile ◽  
Maximum Solubility ◽  
In Vivo Evaluation ◽  
Hydrophobic Nature

Carbamazepine (CBZ) is an antiepileptic drug having low bioavailability due to its hydrophobic nature. In the current study, efforts are made to investigate the effect of dicarboxylic acid coformer spacer groups (aliphatic chain length) on physicochemical properties, relative humidity (RH) stability, and oral bioavailability of CBZ cocrystals. Slurry crystallization technique was employed for the preparation of CBZ cocrystals with the following coformers: adipic (AA), glutaric (GA), succinic (SA), and malonic acid (MA). Powder X-ray diffractometry and Fourier-transform infrared spectroscopy confirmed cocrystal preparation. Physicochemical properties, RH stability, and oral bioavailability of cocrystals were investigated. Among the prepared cocrystals, CBZ-GA showed maximum solubility as well as improved dissolution profile (CBZ-GA > CBZ-MA > CBZ-AA > pure CBZ > CBZ-SA) in ethanol. Maximum RH stability was shown by CBZ-AA, CBZ-SA, and CBZ-MA. In vivo studies confirmed boosted oral bioavailability of cocrystals compared to pure CBZ. Furthermore, in vivo studies depicted the oral bioavailability order of cocrystals as CBZ-GA > CBZ-MA > Tegral® > CBZ-AA > CBZ-SA > pure CBZ. Thus, pharmaceutical scientists can effectively employ cocrystallization technique for tuning physicochemical properties of hydrophobic drugs to achieve the desired oral bioavailability. Overall, results reflect no consistent effect of spacer group on physicochemical properties, RH stability, and oral bioavailability of cocrystals.

scholarly journals Assessment of In Vitro Bioaccessibility and In Vivo Oral Bioavailability as Complementary Tools to Better Understand the Effect of Cooking on Methylmercury, Arsenic, and Selenium in Tuna

Toxics ◽  
2021 ◽  
Vol 9 (2) ◽  
pp. 27
Author(s):  
Tania Charette ◽  
Danyel Bueno Dalto ◽  
Maikel Rosabal ◽  
J. Jacques Matte ◽  
Marc Amyot
Keyword(s):  
Oral Bioavailability ◽  
Fish Muscle ◽  
In Vitro Models ◽  
In Vivo Studies ◽  
In Vivo Models ◽  
Exposure Pathway ◽  
In Vitro Bioaccessibility ◽  
Kinetics Of

Fish consumption is the main exposure pathway of the neurotoxicant methylmercury (MeHg) in humans. The risk associated with exposure to MeHg may be modified by its interactions with selenium (Se) and arsenic (As). In vitro bioaccessibility studies have demonstrated that cooking the fish muscle decreases MeHg solubility markedly and, as a consequence, its potential absorption by the consumer. However, this phenomenon has yet to be validated by in vivo models. Our study aimed to test whether MeHg bioaccessibility can be used as a surrogate to assess the effect of cooking on MeHg in vivo availability. We fed pigs raw and cooked tuna meals and collected blood samples from catheters in the portal vein and carotid artery at: 0, 30, 60, 90, 120, 180, 240, 300, 360, 420, 480 and 540 min post-meal. In contrast to in vitro models, pig oral bioavailability of MeHg was not affected by cooking, although the MeHg kinetics of absorption was faster for the cooked meal than for the raw meal. We conclude that bioaccessibility should not be readily used as a direct surrogate for in vivo studies and that, in contrast with the in vitro results, the cooking of fish muscle did not decrease the exposure of the consumer to MeHg.

scholarly journals DEVELOPMENT AND EVALUATION OF FLOATING TABLET OF METOPROLOL SUCCINATE FOR INCREASED BIOAVAILABILITY VIA IN VIVO STUDY

2019 ◽  
pp. 281
Author(s):  
KAUSER FATEMA ◽  
SADHANA SHAHI
Keyword(s):  
Drug Release ◽  
Oral Bioavailability ◽  
In Vivo Studies ◽  
Physical Parameters ◽  
Metoprolol Succinate ◽  
Sustained Release Formulation ◽  
Dissolution Study ◽  
Floating Tablet

Objective: This study was performed to formulate a floating tablet using hydrophobic glyceryl behenate (GB) and hydrophilic hydroxypropyl methylcellulose polymers, optimization of the same for retention in stomach and sustained drug delivery over a period of 20 h from upper gastrointestinal tract so as to increase its oral bioavailability. Methods: Granules of GB with the metoprolol succinate (MS) was formulated and compressed with the other ingredients to formulate a floating tablet. Physiochemical parameters of an optimized formulation along with its in vitro buoyancy study, dissolution study, in vivo studies in rabbit, and stability studies were performed. Results: Differential scanning calorimetry data show no interaction between polymers and the drug MS. A 32 factorial design was applied for optimization purpose, and from ANOVA and surface response plot the best formulation (F3) was obtained. In vitro dissolution study shows sustained drug release for 20 h for all the formulations and in vivo studies using rabbit model show increased bioavailability of an optimized formulation F3 as compared to the marketed sustained release formulation of MS (25 mg). Stability study shows no comparable differences in physical parameters and the drug release of initial formulation and the one which is kept for accelerated stability testing. Conclusion: Hence, we can conclude that a floating tablet containing a combination of hydrophilic and hydrophobic polymers can be used for gastric retention for more than 20 h which will increase the oral bioavailability of MS.

scholarly journals FORMULATION AND EVALUATION OF OPTIMISED MALTODEXTRIN BASED PRONIOSOME POWDERS CONTAINING BAZEDOXIFENE ACETATE FOR ORAL DELIVERY

2020 ◽  
pp. 56-66
Author(s):  
SMITHA GANDRA
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vivo Studies ◽  
In Vitro Dissolution ◽  
Ionic Surfactant ◽  
Bioavailability Enhancement ◽  
Cholesterol Ratio

Objective: The main objective of the present study was to develop proniosomal formulations to enhance the oral bioavailability of bazedoxifene acetate by improving solubility, dissolution and/or intestinal permeability. Methods: Proniosomal powder formulations were prepared with bazedoxifene acetate drug varying the span 40 and cholesterol ratio in the range of 0.8:0.2 to 0.2:0.8 using maltodextrin as a carrier by slurry method. The prepared proniosomal powder was filled into capsules. The bioavailability enhancement of proniosomes loaded with drug was studied focusing on non-ionic surfactants composition and drug: span 40 ratio. Prepared proniosomes were characterized for their particle size distribution, zeta potential, entrapment efficiency, in vitro dissolution study and thermal characteristics to understand the phase transition behavior. Further, the formulated proniosomes were subjected to stability behavior, ex vivo permeation studies using rat intestine followed by in vivo studies. Results: Physico-chemical studies help in the optimization of formulations. Enhancement in dissolution is due to the incorporation of bazedoxifene acetate into the non-ionic surfactant and change in the physical state from crystalline to amorphous, thus improving oral bioavailability. Ex vivo studies show significant permeation enhancement across the gastrointestinal membrane compared to control. Conclusion: In conclusion, proniosomes provide a powerful and functional way of the distribution of inadequately soluble bazedoxifene acetate drug, which is proved from in vivo studies based on the enhanced oral delivery.

ROSUVASTATIN CALCIUM PRONIOSOME POWDER: A NOVEL APPROACH TO IMPROVE INTESTINAL ABSORPTION AND BIOAVAILABILITY

2020 ◽  
pp. 148-156
Author(s):  
SMITHA GANDRA
Keyword(s):  
Oral Bioavailability ◽  
Oral Delivery ◽  
Ex Vivo ◽  
In Vivo Studies ◽  
In Vitro Dissolution ◽  
Ionic Surfactant ◽  
Bioavailability Enhancement ◽  
Rosuvastatin Calcium

Objective: The main objective of the present study was to develop proniosomal formulations to enhance the oral bioavailability of rosuvastatin calcium by improving solubility, dissolution, and/or intestinal permeability. Methods: Proniosomal powder formulations were prepared with rosuvastatin calcium drug varying the Span 40 and cholesterol ratio in the range of 0.8:0.2–0.2:0.8 using maltodextrin as carrier by slurry method. The prepared proniosomal powder was filled into capsules. The bioavailability enhancement of proniosomes loaded with drug was studied focusing on non-ionic surfactants composition and drug:Span 40 ratio. Prepared proniosomes were characterized for their particle size distribution, zeta potential, entrapment efficiency, in vitro dissolution study, and thermal characteristics to understand the phase transition behavior. Further, the formulated proniosomes were subjected to stability behavior, ex vivo permeation studies using rat intestine followed by in vivo studies. Results: Physicochemical studies help in optimization of formulations. Enhancement in dissolution is due to incorporation of rosuvastatin calcium into the non-ionic surfactant and change in the physical state from crystalline to amorphous, thus improving oral bioavailability. Ex vivo studies show significant permeation enhancement across gastrointestinal membrane compared to control. Conclusion: Proniosomes provide a powerful and functional way of distribution of inadequately soluble rosuvastatin calcium drug which is proved from in vivo studies based on the enhanced oral delivery.

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