Prediction of Oral Drug Absorption in Rats from In Vitro Data

Akiyama, Yoshiyuki; Matsumura, Naoya; Ono, Asami; Hayashi, Shun; Funaki, Satoko; Tamura, Naomi; Kimoto, Tetsuo; Jiko, Maiko; Haruna, Yuka; Sarashina, Akiko; Ishida, Masahiro; Nishiyama, Keisuke; Fushimi, Masahiro; Kojima, Yukiko; Fujita, Takuya; Sugano, Kiyohiko

doi:10.1007/s11095-022-03173-6

Cited by 7 publications

(4 citation statements)

References 88 publications

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“…The differentiated Caco-2 cells exhibit features that closely resemble small bowel enterocytes, including brush-border microvilli [ 228 , 229 ], and produce various cytokines, like IL-6, IL-8, IL-15 and TNF [ 230 , 231 , 232 ]. As such, Caco-2 cells are widely used in IBD research [ 233 , 234 ]. Zhang et al [ 235 ] investigated in vitro anti-inflammatory effects of Paenibacillus polymyxa Prazmowski exopolysaccharide (PYQ1-EPS) on TNF-induced inflammation in Caco-2 cells.…”

Section: Screening Isolated Compounds For Anti-inflammatory Propertiesmentioning

confidence: 99%

Approaches, Strategies and Procedures for Identifying Anti-Inflammatory Drug Lead Molecules from Natural Products

Jamtsho,

Yeshi,

Perry

et al. 2024

Pharmaceuticals

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Natural products (NPs) have played a vital role in human survival for millennia, particularly for their medicinal properties. Many traditional medicine practices continue to utilise crude plants and animal products for treating various diseases, including inflammation. In contrast, contemporary medicine focuses more on isolating drug-lead compounds from NPs to develop new and better treatment drugs for treating inflammatory disorders such as inflammatory bowel diseases. There is an ongoing search for new drug leads as there is still no cure for many inflammatory conditions. Various approaches and technologies are used in drug discoveries from NPs. This review comprehensively focuses on anti-inflammatory small molecules and describes the key strategies in identifying, extracting, fractionating and isolating small-molecule drug leads. This review also discusses the (i) most used approaches and recently available techniques, including artificial intelligence (AI), (ii) machine learning, and computational approaches in drug discovery; (iii) provides various animal models and cell lines used in in-vitro and in-vivo assessment of the anti-inflammatory potential of NPs.

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Section: Screening Isolated Compounds For Anti-inflammatory Propertiesmentioning

confidence: 99%

Approaches, Strategies and Procedures for Identifying Anti-Inflammatory Drug Lead Molecules from Natural Products

Jamtsho,

Yeshi,

Perry

et al. 2024

Pharmaceuticals

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“…Bioavailability testing of SNEDDS was performed using an artificial crane and the Wilson method [28,29]. In this test, 2 ml SNEDDS and 5 ml gastric fluid (pH 3.5) were enclosed in the dialysis membrane.…”

Section: Snedds Bioavailability Testmentioning

confidence: 99%

“…Samples were made at 3 ml each for 24 h with 12 points, and then 4 points that met the peak and steady-state levels were collected. After each sampling, the receiving medium was substituted to maintain sink condition [28,30].…”

Section: Snedds Bioavailability Testmentioning

confidence: 99%

Modifying Fraction Extracted From Sesewanua (Clerodendrum Fragrans Wild) Leaves in Snedds Preparations: Characterization and Bioavailability Test

SAPIUN,

IMRAN,

ASWAD

et al. 2024

Int J App Pharm

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Objective: This study aimed to determine the effect of compound modification using acyl chloride derivatives on n-hexane: ethyl acetate fraction of sesewanua leaves, focusing on the characteristics and pharmacokinetics profile in Self-Nano-emulsifying Drug Delivery System (SNEDDS) preparations. Methods: A quasi-experimental method was used with six SNEDDS formulas, namely F0 (without active substance), F1 (acetyl chloride fraction), F2 (propanoyl chloride fraction), F3 (butyryl chloride fraction), and F4 (pentanoyl chloride fraction) and F5 (piperine compound). The fractions were subjected to characterization tests, including particle size, polydispersity index, and zeta potential as well as determination of pharmacokinetics profile using the modified crane and Wilson method. Results: The results showed that the characterization tests of particle size using Particle Size Analyzer (PSA) for F0-F5 on gastric fluid included 15.8, 17,367, 20,367, 15.8, 28.233, and 21.533 nm. The polydispersity index values were 0.211, 0.438, 0.311, 0.383, 0.394, and 0.397, while the Zeta Potential values were-22,267,-22.2,-23.5,-24,033,-22,967, and-21.6 mV, respectively. The pharmacokinetics profile of AUC0-∞ was as follows: F0 0 μg, F1 492.83, F2 492.83, F3 245.98, F4 492.94, and F5 843.38 μg. Fraction five (F5) as a control had a higher AUC0-∞ value than compared to the fractions modified with acyl chloride derivatives. The T1/2 elimination values were F0 0 h, F1 22.5 h, F2 10.811 h, F3 35.54 h, F4 231.01 h, and F5 15.469 h. Conclusion: Based on the results, the addition of acetyl, propanoyl, butyryl, and penthanoyl chloride affected Particle Size Characterization Analysis and pharmacokinetics profile of SNEDDS preparation of n-hexane: ethyl acetate fraction. Structural modification showed the ability to alter the bioavailability of the active ingredient according to the desired therapeutic goal.

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“…The combination with pharmacodynamics (PD) models further enable describing the response of the studied system to drugs. Given these advantages, PK/PD models have been seen significant adoption to optimise dose and regimen [13], develop effective drugs [14], scale laboratory experiments to clinical trials [15], and explore and examine the physiological barriers in drug delivery [16], particularly the delivery to the central nervous system [17,18]. Unlike PK/PD models, transport-based models are able to accommodate the realistic geometry of the entire tissue or tissue microstructure for outputting both the temporal drug concentration and spatial distribution.…”

Section: Remarksmentioning

confidence: 99%