Article
Chemistry, Applied
Yuying Liu, Siyuan Jiang, Yuxin Xiang, Fengxiang Lin, Xingyu Yue, Minkun Li, Jinjing Xiao, Haiqun Cao, Yanhong Shi
Summary: This study examined the bioavailability and bioaccessibility of pyrethroid pesticides in honey using a mouse bioassay and in vitro methods. The results showed that liver plus kidney data served as a suitable biomarker for estimating relative bioavailability, and there were significant correlations between bioavailability and bioaccessibility. The findings also suggested that the bioavailability of honey can be influenced by the content and physicochemical properties of the nectar plants it comes from. These insights into assessing human exposure to pesticides based on bioavailability can reduce uncertainty in the risk assessment of dietary pesticide exposure.
Review
Chemistry, Multidisciplinary
Tejas Girish Agnihotri, Amit Alexander, Mukta Agrawal, Sunil Kumar Dubey, Aakanchha Jain
Summary: Understanding the interaction between nanoparticles and biological systems is a challenge in nanotherapeutics. Protein corona plays a crucial role in cellular uptake and in vivo behavior of nanoparticles. In vitro dissolution testing and in vitro in vivo correlation (IVIVC) are useful approaches to evaluate the fate of nanoparticles. This review emphasizes the importance of protein corona, factors affecting the interaction, and various dissolution media for different nanocarrier systems, and discusses the limitations and regulatory perspective of IVIVC.
JOURNAL OF CONTROLLED RELEASE
(2023)
Article
Pharmacology & Pharmacy
Haidara Majid, Anke Bartel, Bjoern B. Burckhardt
Summary: This study applied an innovative, standardized, and controlled ex vivo permeation model to evaluate its predictivity for sublingual propranolol absorption data and confirmed it as a viable alternative to animal testing. The model showed good predictivity for pH-dependent permeability and revealed a strong correlation between obtained permeability and reported pharmacokinetic animal data.
EUROPEAN JOURNAL OF PHARMACEUTICS AND BIOPHARMACEUTICS
(2021)
Article
Pharmacology & Pharmacy
Anna Costanzini, Chiara Ruzza, Joaquim Azevedo Neto, Chiara Sturaro, Davide Malfacini, Catia Sternini, Roberto De Giorgio, Girolamo Calo
Summary: Opioid-induced constipation is a common adverse effect of opioid drugs. Naloxegol, a peripherally acting mu opioid receptor antagonist, has been shown to be effective in counteracting the constipating effects of fentanyl in both in vitro and in vivo experiments. Through in vitro and in vivo studies, naloxegol demonstrated competitive mu receptor antagonist properties and useful PAMORA action for treating opioid-induced constipation.
EUROPEAN JOURNAL OF PHARMACOLOGY
(2021)
Review
Chemistry, Multidisciplinary
Amit Dabke, Saikat Ghosh, Pallavi Dabke, Krutika Sawant, Ajay Khopade
Summary: Complex injectable drug products (CIDPs) have complex kinetics and require advanced computational models for accurate prediction of in-vitro-in-vivo correlation (IVIVC). Computational modelling aims to develop formulation strategies for predictable and discriminatory IVIVC, and tools like PBPK modelling have helped in predicting pharmacodynamic parameters. This review highlights the important aspects to be considered in developing a predictive PBPK model for IVIVC.
JOURNAL OF CONTROLLED RELEASE
(2023)
Article
Pharmacology & Pharmacy
Seeprarani Rath, Isadore Kanfer
Summary: The safety and efficacy of a generic medicine can be confirmed by demonstrating bioequivalence between the generic product and its reference listed drug. For topical dermatological products, clinical trials in patients are required. This investigation aimed to predict in vivo performance by correlating in vitro release testing data with tape stripping data following the application of metronidazole creams to the skin.
Article
Pharmacology & Pharmacy
Tuba Incecayir, Muhammed Enes Demir
Summary: This study investigates the in vivo relevance of a biphasic dissolution test for immediate release formulations of lamotrigine, a BCS Class II drug, and demonstrates that the test can accurately estimate the in vivo performance of the drug.
Article
Chemistry, Multidisciplinary
Bo Wan, Quanying Bao, Diane J. Burgess
Summary: The development of in vitro-in vivo correlations (IVIVCs) for complex long-acting parenterals, such as PLGA microspheres, is challenging. This study investigated the impact of PLGA source variation on the development and predictability of IVIVCs for PLGA microspheres. The results showed that different PLGA sources led to significant differences in critical quality attributes and subsequently affected the in vitro and in vivo performance. The study provides a comprehensive understanding of IVIVC development for PLGA microspheres.
JOURNAL OF CONTROLLED RELEASE
(2022)
Article
Pharmacology & Pharmacy
Bo Wan, Quanying Bao, Ruifeng Wang, Diane J. Burgess
Summary: Poly(lactic-co-glycolic acid) (PLGA) plays a significant role in the performance of long-acting parenteral drug products. Due to their large size, charged state, and hydrophilicity, peptide loaded microspheres can exhibit complex release mechanisms, making it challenging to develop in vitro-in vivo correlations (IVIVCs). This study investigated the influence of PLGA source variations on IVIVC development and predictability for peptide loaded PLGA microspheres, and established conventional IVIVCs that were able to predict in vivo performance using in vitro release profiles.
INTERNATIONAL JOURNAL OF PHARMACEUTICS
(2022)
Review
Food Science & Technology
Joanna Nadia, John Bronlund, Rajinder Paul Singh, Harjinder Singh, Gail M. Bornhorst
Summary: This review discusses the physical breakdown of starch-based foods in the mouth and stomach, the quantification of these breakdown processes, and their links to physiological outcomes, such as gastric emptying and glycemic response. It emphasizes that the physical breakdown prior to small intestinal digestion, especially during gastric digestion, should not be neglected in understanding the digestion of solid starch-based foods.
COMPREHENSIVE REVIEWS IN FOOD SCIENCE AND FOOD SAFETY
(2021)
Article
Pharmacology & Pharmacy
D. E. Selley, M. L. Banks, C. M. Diester, A. M. Jali, L. P. Legakis, E. J. Santos, S. S. Negus
Summary: The pharmacodynamic efficacy of drugs in activating their receptors is crucial in determining drug effects. Fixed-proportion mixtures of an agonist and antagonist for a given receptor can be adjusted to precisely control net efficacy of the mixture in activating that receptor. Manipulation of agonist proportion in agonist/antagonist mixtures governs net mixture efficacy at the target receptor.
JOURNAL OF PHARMACOLOGY AND EXPERIMENTAL THERAPEUTICS
(2021)
Article
Plant Sciences
Ji-Hye Jang, Chang-Seob Seo, Hyekyung Ha, Su-Cheol Han, Mee-Young Lee, Hyeun-Kyoo Shin
Summary: Asiasari Radix et Rhizoma (ARE) is a traditional herbal medicine known for its pain-relieving properties, but recent studies suggest that it may have genotoxic effects, particularly evident in chromosomal aberration and Ames tests. Further research is needed to fully understand the potential risks associated with the use of this herbal medicine.
JOURNAL OF ETHNOPHARMACOLOGY
(2021)
Article
Pharmacology & Pharmacy
Mohsen A. Hedaya, Soha M. El-Masry, Sally A. Helmy
Summary: In this study, the in vitro dissolution and in vivo pharmacokinetics of different etamsylate formulations were investigated, leading to the development of a physiological model to establish the IVIVC for controlled release tablets. The developed model showed good agreement between predicted and observed drug profiles, indicating its validity for predicting in vivo dissolution. Overall, the buffer transition method was found to be appropriate for predicting the in vivo dissolution of controlled release matrix tablets.
JOURNAL OF DRUG DELIVERY SCIENCE AND TECHNOLOGY
(2021)
Article
Chemistry, Medicinal
Yuosef Al Ayoub, Asma Buzgeia, Ghadeer Almousawi, Hassan Raza Ali Mazhar, B. Alzouebi, Rajendran C. Gopalan, K. H. Assi
Summary: In vitro dissolution testing is essential in the pharmaceutical industry, and a method for investigating the dissolution profile of inhaled products has been developed. The study modified the Twin Stage Impinger to examine the in vitro-in vivo correlation and enhance the Fine Particle Dose collection method for dry powder inhalers. The results showed that the modified Twin Impinger effectively tested the dissolution rate of drugs. Comparison with actual in vivo pharmacokinetic values validated the effectiveness of this in vitro dissolution method.
JOURNAL OF PHARMACEUTICAL SCIENCES
(2022)
Article
Pharmacology & Pharmacy
Da Young Lee, Soyoung Shin, Tae Hwan Kim, Beom Soo Shin
Summary: This study aimed to establish an extended design of experiment (DoE)-in vitro in vivo correlation (IVIVC) model that defines the relationship between formulation composition, in vitro dissolution, and in vivo pharmacokinetics. By applying a mixture design of DoE and prepared by the wet granulation method, 14 sustained-release (SR) tablets of a model drug, donepezil, were designed and prepared. The in vitro dissolution patterns of donepezil SR tablets were described by Michaelis-Menten kinetics. The predictability of the derived DoE model was validated, and level A IVIVC was established by correlating the in vitro and in vivo V-max. Finally, the extended DoE-IVIVC model was developed, allowing one to predict the maximum plasma concentration (C-max) and the area under the plasma concentration-time curve (AUC) of donepezil SR tablets.