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Yakugaku Zasshi : Journal of the... 2024It is well known that the oral bioavailability of hydrophilic and macromolecular drugs is generally very poor due to their poor membrane permeability characteristics.... (Review)
Review
It is well known that the oral bioavailability of hydrophilic and macromolecular drugs is generally very poor due to their poor membrane permeability characteristics. Among these poorly absorbed drugs, peptide and protein drugs are typical poorly absorbed drugs which have low stability and poor permeability in the gastrointestinal tract. Consequently, the clinical administration of peptide and protein drugs is presently limited to administration by injection. However, such frequent administration subjects the patients to considerable pain, and there is also the possibility of the manifestation of serious side effects. Therefore, various approaches have been examined to overcome the poor absorption characteristics of these drugs. These approaches include (1) to use additives including absorption enhancers and protease inhibitors, (2) to modify the chemical structure of peptide and protein drugs, and (3) to apply dosage forms to these drugs, (4) to develop a novel administration method for these drugs that can serve as an alternative to oral and injection administration. We demonstrated that intestinal and transmucosal absorption of peptide and protein drugs could be improved by using these approaches. These approaches may give us useful basic information to improve the intestinal and transmucosal absorption of peptide and protein drugs.
Topics: Humans; Intestinal Absorption; Peptides; Proteins; Biological Availability; Protease Inhibitors; Permeability; Administration, Oral; Intestinal Mucosa; Dosage Forms
PubMed: 38945845
DOI: 10.1248/yakushi.23-00199 -
Food Research International (Ottawa,... Aug 2024Obesity, a global health crisis, is fueled by shifts in behavior and environmental factors, notably increased consumption of energy-dense processed foods and inadequate...
Obesity, a global health crisis, is fueled by shifts in behavior and environmental factors, notably increased consumption of energy-dense processed foods and inadequate dietary fiber. Traditional weight loss methods pose safety challenges. Sodium carboxymethylcellulose (CMC), a promising dietary fiber supplement, aids weight management. However, CMC-based hydrogels have mechanical weaknesses and poor gastrointestinal retention. A new dual-network structured hydrogel here was introduced to address these issues, maintaining volume and elasticity in the digestive system without adding calories, reducing caloric density, and enhancing food elasticity for prolonged satiety. The study assessed four distinct hydrogels, analyzing their mechanical characteristics under simulated gastrointestinal conditions and biomimetic digestion to identify promising options for clinical development. This dual-network hydrogel exhibits a mechanical strength up to 100 times that of the original gel, while its swelling rate throughout the digestion process is approximately twice that of the original gel. This offers a potential solution for obesity management, providing sustained satiety and addressing the mechanical deficiencies of current hydrogels within the digestive system.
Topics: Hydrogels; Carboxymethylcellulose Sodium; Obesity; Digestion; Humans; Dietary Fiber; Weight Loss; Elasticity
PubMed: 38945596
DOI: 10.1016/j.foodres.2024.114560 -
Food Research International (Ottawa,... Aug 2024More than 40 volatile compounds were detected in sea cucumber powder during the processing (through freeze-dried, desalination, supercritical fluid extraction and...
More than 40 volatile compounds were detected in sea cucumber powder during the processing (through freeze-dried, desalination, supercritical fluid extraction and ultra-micro grinding) by multiple methods including e-nose, GC-IMS and GC-MS. It has been determined that aldehydes are the predominant volatile substances in the original freeze-dried sample, accounting for about 30 % of the total volatile substances. In addition, we established a supercritical fluid extraction strategy that could efficiently remove the aldehydes from the sea cucumber powder. GC-IMS and GC-MS showed that the relative content of aldehydes significantly decreased by 14 % and 28 %, respectively. Quantification of aldehydes using GC-MS showed a significant decrease in octanal from 927 µg/kg to 159 µg/kg. Further investigation combined with OAV analysis showed that 17 volatile substances in the freeze-dried sea cucumber powder were considered to be the predominant volatile compounds (OAV > 1).The primary fishy compounds found in sea cucumber powder were identified as hexanal, octanal, and an unidentified compound using GC-O, which can be effectively removed (OAV can't been estimated) by the supercritical fluid extraction strategy we established.
Topics: Chromatography, Supercritical Fluid; Sea Cucumbers; Volatile Organic Compounds; Animals; Gas Chromatography-Mass Spectrometry; Powders; Food Handling; Freeze Drying; Aldehydes; Electronic Nose; Seafood
PubMed: 38945572
DOI: 10.1016/j.foodres.2024.114603 -
Annales Pharmaceutiques Francaises Jun 2024Nanosuspensions have emerged as a promising avenue in pharmaceutical innovation, particularly for enhancing the bioavailability of poorly soluble medications. This... (Review)
Review
INTRODUCTION
Nanosuspensions have emerged as a promising avenue in pharmaceutical innovation, particularly for enhancing the bioavailability of poorly soluble medications. This article explores the transformative potential of nanosuspensions, emphasizing the critical role of particle size reduction through nanonization techniques. With conventional approaches often falling short in addressing the bioavailability challenges of hydrophobic drugs, nanosuspensions offer multifaceted applications and distinctive advantages in drug delivery.
METHODS
The study delves into various nanosuspension preparation techniques, including high-pressure homogenization, media milling, emulsification-solvent evaporation, precipitation, and supercritical fluid processes. Each method brings unique advantages and limitations, contributing to the expanding repertoire of nanosuspension formulation methods. The article emphasizes the necessity for meticulous planning, evaluation, and ongoing research across different drugs to optimize their use effectively.
RESULTS
Nanosuspensions exhibit versatility in administration routes, spanning parenteral, peroral, ocular, and pulmonary pathways, making them applicable across diverse dosage forms. Current efforts are directed towards furthering their application in site-specific medication administration, indicating their potential in tailored therapeutic strategies. Nanosuspensions offer a promising solution for enhancing drug solubility and bioavailability, addressing the persistent challenge of poor solubility in pharmaceutical compounds.
DISCUSSION
The significance of careful formulation and stabilization using polymers and surfactants is underscored, ensuring the efficacy and safety of nanosuspensions. By discussing the benefits, drawbacks, and nuances of each preparation technique, the article aims to simplify future research endeavors in the field of nanosuspensions. Additionally, a comprehensive overview of nanosuspensions, including their preparation methods, benefits, characterization, patents, marketed products, and intended uses, sheds light on this evolving domain in pharmaceutical sciences.
CONCLUSION
Nanosuspensions represent a promising approach for overcoming bioavailability challenges associated with poorly soluble medications. The article highlights their transformative potential in pharmaceutical innovation, emphasizing the importance of continued research and optimization to harness their benefits effectively. Nanosuspensions offer a viable solution for enhancing drug solubility and bioavailability, with implications for improving therapeutic outcomes in various medical conditions.
PubMed: 38945393
DOI: 10.1016/j.pharma.2024.06.003 -
Journal of Gastrointestinal and Liver... Jun 2024
Topics: Humans; Charcoal; Tablets; Foreign Bodies; Esophagoscopy; Esophagus; Male; Female
PubMed: 38944850
DOI: 10.15403/jgld-5310 -
Lancet (London, England) Jun 2024
Topics: Humans; Budesonide; Glomerulonephritis, IGA; Glucocorticoids; Delayed-Action Preparations
PubMed: 38944527
DOI: 10.1016/S0140-6736(24)00796-7 -
Lancet (London, England) Jun 2024
Topics: Humans; Budesonide; Glomerulonephritis, IGA; Glucocorticoids; Delayed-Action Preparations
PubMed: 38944525
DOI: 10.1016/S0140-6736(24)00795-5 -
Lancet (London, England) Jun 2024
Topics: Humans; Budesonide; Glomerulonephritis, IGA; Glucocorticoids; Delayed-Action Preparations
PubMed: 38944524
DOI: 10.1016/S0140-6736(24)00794-3 -
International Journal of Pharmaceutics Jun 2024Increasing the solubility of drugs is a recurrent objective of pharmaceutical research, and one of the most widespread strategies today is the formulation of...
Increasing the solubility of drugs is a recurrent objective of pharmaceutical research, and one of the most widespread strategies today is the formulation of nanocrystals (NCs). Beyond the many advantages of formulating NCs, their incorporation into solid dosage forms remains a challenge that limits their use. In this work, we set out to load Atorvastatin NCs (ATV-NCs) in a delivery device by combining 3D scaffolds with an "in situ" loading method such as freeze-drying. When comparing two infill patterns for the scaffolds at two different percentages, the one with the highest NCs load was chosen (Gyroid 20 % infill pattern, 13.8 ± 0.5 mg). Colloidal stability studies of NCs suggest instability in acidic media, and therefore, the system is postulated for use as a sublingual device, potentially bypassing stomach and hepatic first-pass effects. An ad hoc dissolution device was developed to mimic the release of actives. The nanometric size and properties acquired in the process were maintained, mainly in the dissolution rate and speed, achieving 100 % dissolution of the content in 180 s. Based on these results, the proof of concept represents an innovative approach to converting NCs suspensions into solid dosage forms.
PubMed: 38944168
DOI: 10.1016/j.ijpharm.2024.124396 -
Bratislavske Lekarske Listy 2024To create a new mucoadhesive dosage form based on PluronicF127 followed by transformation into a gel form upon intranasal administration for targeted delivery to brain...
OBJECTIVES
To create a new mucoadhesive dosage form based on PluronicF127 followed by transformation into a gel form upon intranasal administration for targeted delivery to brain tissueMETHODS: Citicoline, cytidine diphosphocholine, designated as CDP-choline, was purchased as a white powder with the molecular weight of 510.31 g/mol. The triblock copolymers of polyethylene glycol-block-polypropylene glycol-block-polyethylene glycol (PEG-PPG-PEG), branded as Pluronic F127, was used.
RESULTS
When instilled into the nasal cavity, Pluronic F127 for intranasal administration is transformed into a gel that remains retained for 45-55 minutes, which promotes better penetration of drugs into the brain tissue.
CONCLUSION
The polymer's gelling and adhesive properties performed well, which is crucial for further research at the preclinical stage (Tab. 1, Fig. 5, Ref. 28).
Topics: Administration, Intranasal; Poloxamer; Brain; Drug Delivery Systems; Animals; Cytidine Diphosphate Choline; Gels; Polyethylene Glycols; Nasal Mucosa
PubMed: 38943505
DOI: 10.4149/BLL_2024_67