Insight into Fucoidan-based PEGylated PLGA Nanoparticles Encapsulating Methyl Anthranilic Acid: In Vitro Evaluation and In Vivo Anti-inflammatory Study

A potential fucoidan-based PEGylated PLGA nanoparticles (NPs) offering a proper delivery of N-methyl anthranilic acid (MA, a model of hydrophobic anti-inflammatory drug) have been developed via the formation of fucoidan aqueous coating surrounding PEGylated PLGA NPs. The optimum formulation (FuP2) composed of fucoidan:m-PEG-PLGA (1:0.5 w/w) with particle size(365 ± 20.76 nm), zeta potential (-22.30 ± 2.56 mV), % entrapment efficiency (85.45 ± 7.41), drug loading (51.36 ± 4.75 µg/mg of NPs), % initial burst (47.91 ± 5.89), and % cumulative release (102.79 ± 6.89) has been further investigated for the anti-inflammatory in vivo study. This effect of FuP2 was assessed in rats’ carrageenan-induced acute inflammation model. The average weight of the paw edema was significantly lowered (p ≤ 0.05) by treatment with FuP2. Moreover, cyclooxygenase-2 and tumor necrosis factor-alpha immunostaining were decreased in FuP2 treated group compared to the other groups. The levels of prostaglandin E2, nitric oxide, and malondialdehyde were significantly reduced (p ≤ 0.05) in the FuP2-treated group. A significant reduction (p ≤ 0.05) in the expression of interleukins (IL-1b and IL-6) with an improvement of the histological findings of the paw tissues was observed in the FuP2-treated group. Thus, fucoidan-based PEGylated PLGA–MA NPs are a promising anti-inflammatory delivery system that can be applied for other similar drugs potentiating their pharmacological and pharmacokinetic properties

Assessment of oral solid dosage forms administration manner and acceptability

Taking oral solid dosage forms (OSDFs) safely and effectively is particularly important. This study aimed to determine the pattern and knowledge about the proper criteria of OSDF administration and the consumers’ preferences toward OSDF characteristics. The aims of this study were achieved by cross-sectional survey through open and closed-ended questionnaires, and the presence of the main OSDF administration recommendations of a sample of 32 OSDF drug leaflets was assessed. Based on a simple random sample of 250 volunteers, we found inadequate compliance with the OSDF medicine administration criteria. We also found an absence of the main recommendations of OSDF drug administration on most of the investigated OSDF drug leaflets. Conventional white, round tablets were found to be the most preferred type of OSDF drug. These findings can be valuable to pharmaceutical manufacturers, regulatory agencies, and pharmacists to enhancing patient awareness and compliance with OSDF administration for safe and effective drug administration

Comparison of the Rupture and Disintegration Tests for Soft-Shell Capsules

The USP General Chapter < 2040 > Disintegration and Dissolution of Dietary Supplements introduced a rupture test as a performance test of soft-shell capsules. Traditionally, the disintegration test was used for determining the disintegration time of all solid oral dosage forms. The aim of this investigation was to investigate differences between the rupture test and the disintegration test using soft-shell capsules. Five different soft-shell capsule products were chosen based on their filling contents and treated to simulate a production deficiency. The study design compared capsules as received with capsules that were treated by coating them with the liquid contents of another capsule. The capsules were incubated at room temperature and at 40 degrees C. The tests were repeated after two weeks, and at each time point, twelve capsules of each product were tested using the rupture and the disintegration tests. Six capsules were tested untreated, while the other six capsules were treated. Rupture and disintegration times were recorded as dependent variables in each experiment. Thedata were analyzed using ANOVA. According to the USP definition for disintegration, the rupture of a soft-shell capsule can be seen as fulfilling the disintegration criterion if the capsule contents is a semisolid or liquid. Statistical analysis showed no advantage of the rupture test over the disintegration test. On a product-by-product basis, both tests were sensitive to certain investigated parameters. A noticeable difference between both tests was that in most cases, the rupture test reached the defined endpoint faster than the disintegration test. Soft-shell capsules that are subject to a Quality by Design approach should be tested with both methods to determine which performance test is the most appropriate test for a specific product.United States Pharmacopeia, Banner Pharamcaps, Sotax USADrug Development and Innovation Centre at the University of Albert

Insight into Fucoidan-Based PEGylated PLGA Nanoparticles Encapsulating Methyl Anthranilic Acid: In Vitro Evaluation and In Vivo Anti-Inflammatory Study

A potential fucoidan-based PEGylated PLGA nanoparticles (NPs) offering a proper delivery of N-methyl anthranilic acid (MA, a model of hydrophobic anti-inflammatory drug) have been developed via the formation of fucoidan aqueous coating surrounding PEGylated PLGA NPs. The optimum formulation (FuP2) composed of fucoidan:m-PEG-PLGA (1:0.5 w/w) with particle size (365 &plusmn; 20.76 nm), zeta potential (&minus;22.30 &plusmn; 2.56 mV), % entrapment efficiency (85.45 &plusmn; 7.41), drug loading (51.36 &plusmn; 4.75 &micro;g/mg of NPs), % initial burst (47.91 &plusmn; 5.89), and % cumulative release (102.79 &plusmn; 6.89) has been further investigated for the anti-inflammatory in vivo study. This effect of FuP2 was assessed in rats&rsquo; carrageenan-induced acute inflammation model. The average weight of the paw edema was significantly lowered (p &le; 0.05) by treatment with FuP2. Moreover, cyclooxygenase-2 and tumor necrosis factor-alpha immunostaining were decreased in FuP2 treated group compared to the other groups. The levels of prostaglandin E2, nitric oxide, and malondialdehyde were significantly reduced (p &le; 0.05) in the FuP2-treated group. A significant reduction (p &le; 0.05) in the expression of interleukins (IL-1&beta; and IL-6) with an improvement of the histological findings of the paw tissues was observed in the FuP2-treated group. Thus, fucoidan-based PEGylated PLGA&ndash;MA NPs are a promising anti-inflammatory delivery system that can be applied for other similar drugs potentiating their pharmacological and pharmacokinetic properties

Insight into Fucoidan-based PEGylated PLGA Nanoparticles Encapsulating Methyl Anthranilic Acid: In Vitro Evaluation and In Vivo Anti-inflammatory Study

A potential fucoidan-based PEGylated PLGA nanoparticles (NPs) offering a proper delivery of N-methyl anthranilic acid (MA, a model of hydrophobic anti-inflammatory drug) have been developed via the formation of fucoidan aqueous coating surrounding PEGylated PLGA NPs. The optimum formulation (FuP2) composed of fucoidan:m-PEG-PLGA (1:0.5 w/w) with particle size(365 ± 20.76 nm), zeta potential (-22.30 ± 2.56 mV), % entrapment efficiency (85.45 ± 7.41), drug loading (51.36 ± 4.75 µg/mg of NPs), % initial burst (47.91 ± 5.89), and % cumulative release (102.79 ± 6.89) has been further investigated for the anti-inflammatory in vivo study. This effect of FuP2 was assessed in rats’ carrageenan-induced acute inflammation model. The average weight of the paw edema was significantly lowered (p ≤ 0.05) by treatment with FuP2. Moreover, cyclooxygenase-2 and tumor necrosis factor-alpha immunostaining were decreased in FuP2 treated group compared to the other groups. The levels of prostaglandin E2, nitric oxide, and malondialdehyde were significantly reduced (p ≤ 0.05) in the FuP2-treated group. A significant reduction (p ≤ 0.05) in the expression of interleukins (IL-1b and IL-6) with an improvement of the histological findings of the paw tissues was observed in the FuP2-treated group. Thus, fucoidan-based PEGylated PLGA–MA NPs are a promising anti-inflammatory delivery system that can be applied for other similar drugs potentiating their pharmacological and pharmacokinetic properties

Provisional Biopharmaceutical Classification of Some Common Herbs Used in Western Medicine

The aim of this study was to classify some markers of common herbs used in Western medicine according to the Biopharmaceutical Classification System (BCS). The BCS is a scientific approach to classify drug substances based upon their intestinal permeability and their solubility, at the highest single dose used, within the physiologically relevant pH ranges. Known marker components of twelve herbs were chosen from the USP Dietary Supplement Compendium Monographs. Different BCS parameters such as intestinal permeability (P-eff) and solubility (C-s) were predicted using the ADMET Predictor, which is a software program to estimate biopharmaceutical relevant molecular descriptors. The dose number (D-0) was calculated when information from the literature was available to identify an upper dose for individual markers. In these cases the herbs were classified according to the traditional BCS parameters using Peff and Do. When no upper dose could be determined, then the amount of a marker that is just soluble in 250 mL of water was calculated. This value, M-x, defines when a marker is changing from highly soluble to poorly soluble according to BCS criteria. This biopharmaceutically relevant value can be a useful tool for marker selection. The present study showed that a provisional BCS classification of herbs is possible but some special considerations need to be included into the classification strategy. The BCS classification can be used to choose appropriate quality control tests for products containing these markers. A provisional BCS classification of twelve common herbs and their 35 marker compounds is presented.Simulations PlusSimulations PlusHigh Ministry of Education of the Kingdom of Saudi ArabiaHigh Ministry of Education of the Kingdom of Saudi Arabi