The contemplation of amylose for the delivery of ulcerogenic nonsteroidal anti-inflammatory drugs.

This manuscript proposes an innovative approach to mitigate the gastrointestinal adversities linked with nonsteroidal anti-inflammatory drugs (NSAIDs) by exploiting amylose as a novel drug delivery carrier. The intrinsic attributes of V-amylose, such as its structural uniqueness, biocompatibility and biodegradability, as well as its capacity to form inclusion complexes with diverse drug molecules, are meticulously explored. Through a comprehensive physicochemical analysis of V-amylose and ulcerogenic NSAIDs, the plausibility of amylose as a protective carrier for ulcerogenic NSAIDs to gastrointestinal regions is elucidated. This review further discusses the potential therapeutic advantages of amylose-based drug delivery systems in the management of gastric ulcers. By providing controlled release kinetics and enhanced bioavailability, these systems offer promising prospects for the development of more effective ulcer therapies.

Anticancer and chemopreventive potential of Morinda citrifolia L. bioactive compounds: A comprehensive update.

Morinda citrifolia L., commonly known as Noni, has a longstanding history in traditional medicine for treating various diseases. Recently, there has been an increased focus on exploring Noni extracts and phytoconstituents, particularly for their effectiveness against cancers such as lung, esophageal, liver, and breast cancer, and their potential in cancer chemoprevention. This study aims to provide a comprehensive review of in vitro and in vivo studies assessing Noni's impact on cancer, alongside an exploration of its bioactive compounds. A systematic review was conducted, encompassing a wide range of scientific databases to gather pertinent literature. This review focused on in vitro and in vivo studies, as well as clinical trials that explore the effects of Noni fruit and its phytoconstituents-including anthraquinones, flavonoids, sugar derivatives, and neolignans-on cancer. The search was meticulously structured around specific keywords and criteria to ensure a thorough analysis. The compiled studies highlight Noni's multifaceted role in cancer therapy, showcasing its various bioactive components and their modes of action. This includes mechanisms such as apoptosis induction, cell cycle arrest, antiangiogenesis, and immune system modulation, demonstrating significant anticancer and chemopreventive potential. The findings reinforce Noni's potential as a safe and effective option in cancer prevention and treatment. This review underscores the need for further research into Noni's anticancer properties, with the hope of stimulating additional studies and clinical trials to validate and expand upon these promising findings.

Honokiol and its analogues as anticancer compounds: Current mechanistic insights and structure-activity relationship.

Lignans are plant-derived polyphenolic compounds with a plethora of biological applications. Also, regarded as phytoestrogens, the lignans offer a variety of health benefits of which the anti-cancer effects are the most attractive. Honokiol is a lignan isolated from various parts of trees belonging to the genus Magnolia. The bioactivity of honokiol is attributed to its characteristic physical properties, which include small size and the presence of two phenolic groups that may interact with proteins in cell membranes via hydrophobic interactions, aromatic pi orbital co-valency, and hydrogen bonding. The hydrophobicity of honokiol enables its rapid dissolution in lipids and the crossing of physiological barriers, including the blood-brain barrier and cerebrospinal fluid. These factors contribute towards the high bioavailability of honokiol which further support its candidature in medicinal research. Therefore, the anticancer properties of honokiol are of particular interest as many of the contemporary anticancer drugs suffer from bioavailability drawbacks, which necessitates the identification and development of novel candidate molecules directed as anticancer chemotherapeutics. The antioncogenic profile of honokiol also arises from the regulation of various signalling pathways associated with oncogenesis, arresting of the cell cycle by regulation of cyclic proteins, upregulation of epithelial markers and downregulation of mesenchymal markers leading to the inhibition of epithelial-mesenchymal transition, and preventing the metastasis by restricting cell migration and invasion due to the downregulation of matrix-metalloproteinases. In this review, we discuss the anticancer properties of honokiol.

Targeted delivery of fenamates with aminated starch.

Aim: To develop controlled-release tablets based on aminated starch. Materials & methods: Aminated starch was characterized with Fourier transform infrared and x-ray diffraction. Thermogravimetric analysis confirmed the preferential oxidation of crystalline region of starch. Results: The tablets achieved an initial fast release of fenamates, which slows down after 12 h. Drug release was not completed in the simulated intestinal media, which may be due to the stability of imine bond in aminated starch at weakly acidic pH. Drug release was completed in simulated acidic media due to the hydrolysis of imine functionality at strongly acidic pH. Conclusion: Aminated starch with an imine functionality may serve as intestine targeted, controlled drug-delivery system. Mucoadhesive potential of tablets further supports this observation.

Targeted delivery of flufenamic acid by V-amylose.

Aim: Controlled release of flufenamic acid by helical V-amylose to achieve enzyme-responsive, targeted release of the cargo drug. Materials & methods: Solid-state cross-polarization magic angle spinning carbon-13 nuclear magnetic resonance (CP/MAS NMR), Fourier transform IR and x-ray diffraction (XRD) analysis validated the entrapment of flufenamic acid inside the helical structure of V-amylose. Scanning electron microscopy (SEM) investigations established the morphology of conjugates in simulated gastric environment (pH 1.2) and simulated intestine media (pH 7.2) containing hydrolyzing enzyme. Results & discussion: V-amylose-flufenamic acid complex displayed a sustained release of flufenamic acid for 12 h with a marked stability in simulated gastric pH, while showing a controlled release of drug in simulated intestine media. Conclusion: The V-amylose-flufenamic acid system achieves intestine-targeted delivery of flufenamic acid. The controlled release of flufenamic acid may ensure minimal ulcerogenicity and application as enteric coatings.

Therapeutic delivery with V-amylose.

The helical structure of V-amylose offering a superior encapsulation affinity compared with the other polysaccharides, especially toward the amphiphilic or hydrophobic molecules; in addition to providing a higher resistance toward enzymatic hydrolysis support its applications as a potential drug delivery vehicle. Mainly, the glycosidic linkages and -CH2 - groups forming the hydrophobic cavity of V-amylose helix, and the glycosyl hydroxyl groups constituting its hydrophilic periphery promote the loading of a diverse range of molecules via van der Waals forces and hydrogen bonding interactions. These properties enable a high-loading efficiency, targeted delivery, and controlled release of the cargo drug molecules by V-amylose. Besides, V-amylose presents characteristics of an ideal drug delivery system, such as biocompatibility, physiological benevolence, nonimmunogenicity, and biodegradability. The V-amylose polysaccharide chains fold into left-handed single helix comprising of six glucose units in each turn having a pitch height of 7.91-8.17 Å. These structural features of V-amylose differentiate it from the parent amylose polysaccharide and enable the accommodation and nanoencapsulation of a wide range of therapeutics in the former. The tightly packed helical structure of V-amylose provides extraordinary resistance toward digestion by amylase compared with the linear polysaccharides, which supports the application of V-amylose as controlled drug release systems. The activity of the amylase enzyme produced by salivary glands, pancreas, gastrointestinal tract, and gut microbiota on amylose-based drug delivery vehicles promote enzyme-sensitive controlled oral and colon-specific release of the encapsulated drug. The single helical V-amylose with hydrophobic core and hydrophilic periphery forms inclusion complexes that improve the absorption and permeation of drugs having a high clogP index. The present commentary highlights the distinguished features of V-amylose as an imminent drug delivery system.