Formulation Strategies Research Articles

Investigating a novel therapeutic composition for dry eye syndrome management: In vitro and in vivo studies

Dry eye syndrome (DES) presents a significant challenge in ophthalmic care, necessitating innovative approaches for effective management. This research article introduces a multifaceted strategy to address DES through the development of ocular inserts utilizing advanced technologies such as hot-melt extrusion (HME) and the CaliCut post-extrusion system. The formulation includes key ingredients targeting different layers of the tear film and associated inflammation, including hydroxypropyl cellulose (HPC), polyethylene glycol (PEG), castor oil, and dexamethasone. The study incorporates a Design of Experiments (DoE) approach, integrating HME and the precise stretching and cutting technique of CaliCut for manufacturing consistency and dimensional control of the inserts. The developed insert(s) have been systematically characterized for their physicochemical properties, release profile, and in vivo efficacy. In silico molecular docking studies have also been conducted to assess the binding affinities of formulation components with ocular mucin, elucidating their binding affinities. Preliminary results demonstrate promising potential for the developed insert in managing DES, offering preservative-free treatment, sustained drug delivery, and improved patient compliance. This study highlights the integration of advanced technologies and formulation strategies in ocular drug delivery for effective DES management.

Increasing resilience and selection of a strategy for restoring transport networks in extreme natural processes

Aim. The development of an approach to increasing resilience by selecting strategies for restoring transport networks affected by extreme natural processes. Methods. This study evaluates the dynamics of extreme natural processes, specifically exogenous geological processes that can that can disrupt transport networks. It includes as framework for assessing the sustainability and restoration of transport networks under climate risk factors. Strategies for restoring the transport network were formulated. Results. The formulated strategies enable network modeling of transport network topology, which can be represented as an undirected weighted graph with a set of nodes and edges. The proposed model allows determining the most effective strategy for quickly restoring the connectivity of the transport network by determining the optimal sequence of restoration for repairing road sections, considering restoration time. The efficiency of restoring damaged sections of the transport network is expected to decrease as the share of the restored network increases. Therefore, it is crucial to estimate the necessary extend of network restoration to perform the necessary extent of network restoration to support emergency and urgent tasks by RSChS formations in specific areas. Conclusion. The analysis and assessment of alternative solutions for restoring the sustainability of transport networks considers the complexity of tasks under climate risk factors, such as extreme natural processes. In some cases, the RSChS problems do not require complete network restoration, unlike the tasks solved by the transport industry. This work aims to develop a framework for assessing restoration strategies, identifying the features of each of the considered strategies under uncertainty, and increasing operational sustainability. The proposed approach is flexible, allowing decision makers to assess various priorities during a specific natural emergency in a certain area, such as average recovery time, process efficiency, and uncertainty levels, when choosing the most desirable strategy. It is assumed that the average recovery time does not differ significantly among strategies for full network restoration. However, for partial restorations necessary for RSChS tasks, the average restoration time depends on the chosen strategy.

Formulation of protein-loaded nanoparticles via freeze-drying.

Several nanotechnology-based formulation strategies have been reported for the oral administration of biological drugs. However, a prerequisite often overlooked in developing these formulations is their adaptation to a solid dosage form. This study aimed to incorporate a freeze-drying step, using either mannitol or sucrose laurate (SLAE), into the formulation of new insulin-zinc nanocomplexes to render them resistant to intestinal fluids while maintaining a high protein loading. The resulting freeze-dried insulin-zinc nanocomplexes exhibited physicochemical properties consistent with the target product profile, including a particle size of ∼ 100nm, a zeta potential close to neutrality (∼ -15 mV) and a high association efficiency (> 90%). Importantly, integrating the freeze-drying step in the formulation significantly improved the colloidal stability of the system and preserved the stability of the insulin molecules. Results from in vitro and in vivo studies indicated that the insulin activity remained fully retained throughout the entire formulation and freeze-drying processes. In brief, we present a novel protein formulation strategy that incorporates a critical freeze-drying step, resulting in a dry powder enabling efficient protein complexation with zinc and optimized for oral administration.

Implementation of Strategic Management in Optimizing Merdeka Curriculum

This study aims to describe and analyze the implementation of strategic management in optimizing Merdeka Curriculum at SMA Negeri 3 Unggulan Kayuagung. This study uses qualitative methods. It shows that Implementation of strategic management consists of strategy formulation (environmental analysis, vision, mission, goals, targets and strategies), implementation (operational curriculum, programs, monitoring and communication systems, school resources, organizational structure, school’s principal leadership, and work culture), and strategy evaluation. The obstacles are dynamic policies, limited time, work completion gaps, inconsistency, and evaluation document. The solutions are to optimize growth mindset, digitalization; priority scale-based work plans; collaboration culture; performance work management; evaluation instruments and action plans. Novelty of this study resides in the research setting that implements the Merdeka Curriculum with Mandiri Berbagi category, so this study can contribute to strengthening strategic management in educational units to achieve optimal results in facing changes in the Merdeka Curriculum category options.

Physico-chemical Characterisation of Self-Emulsifying Microemulsion of Antimalarial.

Emulsions are employed as drug carriers in pharmaceutical formulations, particularly because they can increase the oral bioavailability of poorly absorbed medications.1 One of the most often used techniques to improve the oral bioavailability of medications, particularly anti-malarial ones, is the use of lipid-based drug delivery. The current research study focuses on using the lipid-based formulation strategy, i.e., self-emulsifying micro emulsions to formulate such anti-malarial drugs and characterise them to study their stability so that the possibility of bioavailability can be studied more. The current research emphasizes on characterisation techniques like transmission electron microscopy (TEM), turbidity index (%TI) and globule size determination as simpler and industrially implacable techniques to study the stability of the self-emulsifying properties of such formulations. In-order to obtain stable formulations with self-emulsifying behaviour the most important factors like the concentrations of surfactants and co-surfactants were one of the variables which were varied in-order to observe their effect on the overall stability of the microemulsions. This research is a step towards the usage of self-emulsifying microemulsions of anti-malarial drugs, for enhancement of oral bioavailability and encourages other researches to use this formulation strategy to improve bioavailability.

New Pipeline for Analysing Fruit Proteolytic Products Used as Digestive Health Nutraceuticals

Proteolytic products are extensively used in the nutraceutical sector to improve protein digestion and muscle quality in target populations (e.g., athletes or elderly). These products are processed using techniques that often lead to low purity but competitive pricing. Despite their widespread use and well-established production methods, the industry lacks standardized analytical methods for assessing these products and detecting potential fraud. This study proposes a comprehensive and harmonized pipeline for their analysis, which includes quantifying total soluble protein and proteolytic activity, as well as the determination of product stability and protein profile using SDS-PAGE and proteomic techniques. Despite the fact that protease extracts from pineapple had the highest protein content, most of the bromelain remained inactive, unlike in kiwi and papaya. SDS-PAGE revealed partial protein degradation of pineapple extracts, whereas kiwi extracts reflected a lower purification level but a higher protein integrity. The application of proteomic approaches strengthened the identification and origin tracing of the proteases. This study contributes to the development of a robust framework for analyzing proteolytic extracts, spanning from soluble protein quantification to protein profiling and activity determination. It may also ensure reliable supplier selection, high-quality manufacturing practices, and the implementation of optimal storage and formulation strategies in the nutraceutical industry.

Advancing Glaucoma Therapy by Exploring the Efficacy and Potential of Brimonidine Niosomal Gel

Glaucoma is a leading cause of permanent vision loss worldwide and is characterised by progressive optic neuropathy with elevated intraocular pressure (IOP) as a major risk factor. Although successful, the current therapeutic strategies are often severely limited by their need for chronic dosing, systemic side effects and poor patient compliance. Brimonidine, an alpha-2 adrenergic receptor agonist which acts selectively, has been beneficial through its IOP-lowering effects by diminishing aqueous humor production and improving uveoscleral outflow. A novel medication delivery technology to enhance ocular bioavailability and extended drug release is brimonidine, formulated as a niosomal gel. The aim of this study is to highlight its clinical efficacy, formulation strategies and mechanism of action that significantly improved glaucoma therapy. Key studies illuminate its potential benefits in reducing dosing frequency, avoiding side effects and increasing patient compliance. Additional study and optimization required to scale-up manufacturing or ensure long-term stability. Possible future directions: combination medications and delivery systems personalized medicine possible future directions in the treatment of glaucoma might include combination medicines and personalized medicine techniques tailored to patient-specific needs. Brimonidine niosomal gel may be a new approach for glaucoma management and it can change the concept of intraocular drug delivery in the future.

Determination of mometasone furoate solubility, using deep eutectic systems, and topical formulation- experimental and computational studies

The low solubility of some drugs in aqueous medium, is currently a challenge for the pharmaceutical industry, affecting drug bioavailability and treatment efficacy, so there is the need to find new solutions for this challenge. In this work, the solubility of a glucocorticoid drug, mometasone furoate (MF), in different deep eutectic systems (DES) is studied. DES present the advantage of being sustainable solvents, which can be used directly in the final formulation, and establish a synergistic effect with the drug. The solubility of MF in different DES is increased, when compared to the solubility of this drug in an aqueous medium, particularly in DES composed by levulinic acid and terpenes such as menthol and thymol, where the solubility of MF was of 24.1 and 103.3 mgMF/gDES, respectively. Solubility was also assessed using the computational determination of the Hansen solubility parameters of MF in these DES, in particular the total solubility parameter (δT) and Relative Energy Difference (RED). The obtained results correlate well with the MF measured experimentally, showing that this computational tool can be further used to predict MF solubility in DES. Furthermore, oil-in-water emulsions containing DES with MF were developed, allowing more versatility compared to the drug in powdered form, and were prepared containing 1 and 5 % of DES with MF. This work highlights that DES can have an important role in drug solubilization and in the development of new formulation strategies for the pharmaceutical industries.

Enzymatic interlocking aptamer-micelles for enhanced cellular internalization and nucleus-targeted cancer phototherapy

Multifunctional micelles that permit both diagnosis and treatment present enormous advantage and potential for precision medicine. However, the inherent complexities and structural instability of these systems often cause unsatisfactory targeting and therapeutic performances. Herein, by ingenious design of a 2,5-bis(2-thienyl)pyrrole (SNS) modifier to covalently link with AS1411 aptamer and lipid segment, a simple strategy is proposed for one-step enzymatic preparation of interlocked aptamer-micelle (IApM) under bio-friendly conditions. The interlocked poly(SNS) skeleton in IApM can not only stabilize the micelle structure but also enhance near-infrared (NIR) absorption ability, thus further enhancing cellular internalization and photothermal therapy. In addition, the multivalent AS1411 aptamers tethered in the hydrophilic shell can simultaneously increase the specific binding affinity of DNA micelles and induce nucleus-targeted accumulation for DNA damage-triggered apoptosis. This DNA micelle achieves “best of both worlds” with enhanced biostability for cellular internalization and improved NIR photothermal conversion efficiency for nucleus-targeted therapy, which provides a promising formulation strategy for precision cancer treatment.

Development and characterization of orodispersible films containing amlodipine besylate and rosuvastatin calcium based on electrospun fibers

Amlodipine besylate (AML) and rosuvastatin calcium (ROS) are commonly used in the treatment of cardiovascular diseases such as hypertension, dyslipidemia, and coroner artery disease. Orodispersible films (ODFs) have received considerable attention in pharmaceutical development studies as they significantly improve patient compliance. The aim of this study was to develop an ODF formulation containing AML and ROS simultaneously as an electrospun fiber fixed dose preparation. Polymer solutions were evaluated for surface tension, viscosity, and conductivity properties. Preformulation studies were conducted to optimize the electrospinning process. Two different formulations, designated ODF-1 and ODF-2 were the focus of this study. Fiber characterization studies, such as scanning electron microscopy (SEM), Fourier transform-infrared spectroscopy (FT-IR), mechanical properties were performed to assess these two formulations. Furthermore, ODF characterizations, such as disintegration and wetting time, homogeneity of contents, and in vitro dissolution studies were carried out. All formulations exhibited suitable mechanical properties, facilitating easy storage and handling. ODF characterizations revealed rapid disintegration and wetting times for all formulations with over 90 % dissolution in 5 min for both AML and ROS. The overall evaluation of all experiments suggests that ODF-1 may more desirable mechanical properties and a more stable dissolution profile compared to ODF-2. Furthermore, individual ODFs loaded with AML or ROS (AML-ODF-1 and ROS-ODF-1) were prepared by ODF-1 preparation method and then characterized to compare the results with fixed dose ODF results. In conclusion, a promising formulation strategy has been developed to obtain an electrospun fiber ODF formulation containing AML and ROS that is reproducible and suitable for industrial production.

Nanoemulgel: A Comprehensive Review of Formulation Strategies, Characterization, Patents and Applications

<p>Background: Delivering hydrophobic or poorly soluble drugs has become increasingly challenging, with issues like stability and bioavailability complicating the process. Among various strategies devised to address these problems, nanoemulgels have proven effective. Nanoemulgels combine a gel base and an emulsion at the nanoscale, making them excellent for drug delivery. The nanoemulsion component protects the active ingredient from degradative reactions like hydrolysis and enzymatic degradation. Meanwhile, the gel base enhances the emulsion's thermodynamic stability by increasing the viscosity of the aqueous phase and reducing surface and interfacial tension. </p><p> Objective: The primary objective of this review was to explore nanoemulgels as a drug delivery system in the pharmaceutical industry. It delves into the advantages and applications of nanoemulgels in various medical fields, compares them with conventional emulgel, and examines formulation strategies, preparation methods, patent trends, future prospects, and evaluation methods in detail. </p><p> Method: An exhaustive literature survey was conducted keeping in view the various aspects of nanoemulgel. Information from various resources, such as books, review articles, scientific reports, research articles, and patents, were searched, read, analyzed, and summarized. </p><p> Conclusion: This review article thoroughly examines nanoemulgels, discussing their formulation strategies, characterization techniques, and applications in various fields. It highlights their benefits, such as enhanced drug solubility, controlled release, improved stability, and targeted delivery. The article also covers patents related to nanoemulgel technology and explores its future prospects, emphasizing potential applications in pharmaceuticals, cosmetics, dermatology, and other industries.</p>

Exploring Astaxanthin-Loaded Nanoformulations for Skin Targeting: Present Progress and Prospective Directions

This comprehensive review provides information on astaxanthin-loaded topical nanocarrier- based formulations for targeted skin enhancement. Astaxanthin, a potent carotenoid derived from microalgae, has garnered considerable attention for its multifaceted potential in skincare, particularly when incorporated into nanocarriers. These nanocarriers, like nanoemulsions, micelles, hydrogels and nanoparticles, have revolutionized the field of dermatology by providing innovative solutions to overcome the limitations associated with astaxanthin's solubility and stability. Astaxanthin's exceptional antioxidant properties, including its ability to neutralize free radicals within both lipid and aqueous environments, make it a compelling bioactive ingredient for combatting oxidative stress, a central contributor to skin aging and various dermatological conditions. The nanoscale size of these carriers facilitates enhanced skin penetration, controlled release, and improved bioavailability, thereby augmenting astaxanthin's therapeutic efficacy. This review meticulously explores the mechanistic insights behind astaxanthin's enhanced delivery and its multifaceted benefits, including photoprotection, anti-inflammatory effects, and wound healing properties. The diverse applications of astaxanthin-loaded nanocarriers in skincare, spanning anti-aging formulations, UV protection, scar healing, and wound repair, are elucidated. Safety considerations are also addressed, drawing from an extensive analysis of preclinical and clinical studies. The review provides valuable insights into optimal concentrations, formulation strategies, and regulatory aspects governing astaxanthin-loaded nanocarriers in skincare products.

Liposomal Drug Delivery for Neurological Disorders: Advances and Challenges

Abstract: Liposomal drug delivery methods are becoming increasingly viable options for improving treatment outcomes for neurological illnesses. These systems provide a flexible framework for the formulation of medications intended for delivery to the brain, protecting the medication from enzymatic breakdown and enhancing its bioavailability. To maximize liposome-drug interactions and improve brain-targeted delivery efficiency, a variety of formulation strategies are used, such as surface modification and remote loading. By utilizing various pathways to cross the blood- -brain barrier (BBB), such as passive diffusion and receptor-mediated transcytosis, liposomes facilitate the effective transport of therapeutic drugs to the brain parenchyma. Liposomal formulations show potential for targeted drug delivery, reducing off-target effects, and improving treatment efficacy in neurological conditions like Parkinson's disease, Alzheimer's disease, stroke, multiple sclerosis, and brain cancers. For instance, in Parkinson's disease, liposomal delivery of neuroprotective agents can help maintain dopamine levels and protect dopaminergic neurons. In Alzheimer's disease, liposomes can be engineered to deliver drugs that reduce amyloid-beta plaques or tau tangles. For brain cancer, liposomal chemotherapy can target tumor cells more precisely while minimizing damage to surrounding healthy tissue. In stroke, liposomal delivery of neuroprotective agents can reduce the extent of brain damage, while in multiple sclerosis, liposomes can be used to deliver drugs that modulate the immune response. However, the clinical translation of liposomal drug delivery systems for brain diseases faces challenges related to scalability, stability, and immunogenicity, in addition to regulatory barriers. Scalability issues arise from the complex manufacturing processes required to produce liposomes consistently on a large scale. Stability concerns involve maintaining the integrity of liposomes during storage and after administration. Immunogenicity can be a problem if the liposomes trigger an unwanted immune response, potentially reducing their effectiveness or causing adverse effects. To overcome these obstacles, multidisciplinary cooperation is essential. Collaboration among materials scientists, pharmacologists, neurologists, and regulatory experts can drive the development of more robust liposomal formulations. Continuous research is needed to refine liposome designs, such as by optimizing lipid composition, surface charge, and size to improve stability and targeting capabilities. Advanced techniques like PEGylation (coating liposomes with polyethylene glycol) can help reduce immunogenicity and extend circulation time in the bloodstream. Despite these challenges, liposomal methods present intriguing prospects for transforming medication administration to the brain and offering effective treatments for neurological illnesses. The development of more sophisticated liposomal technologies, combined with a deeper understanding of their mechanisms of action, could lead to significant breakthroughs in the treatment of neurological disorders. For example, research into ligand- targeted liposomes, which use specific molecules to bind to receptors on the BBB, holds promise for enhancing delivery specificity and efficiency. To fully realize the therapeutic promise of these novel drug delivery systems, further advancements in liposomal technologies and a deeper understanding of their mechanisms are necessary. This includes not only technical improvements but also comprehensive preclinical and clinical studies to evaluate safety, efficacy, and long-term effects. As our knowledge expands and technology progresses, liposomal drug delivery could become a cornerstone of neurological disease treatment, providing new hope for patients with previously intractable conditions.

The Langmuir-Blodgett trough (Langmuir film balance) can be used to understand the stabilizer concentrations in aqueous nano- and microsuspensions

Aqueous suspensions of poorly soluble, crystalline drug particles in the sub-micron range hold the ability to regulate the drug release for a defined period of time after e.g., intramuscular, or subcutaneous administration, working as an eminent formulation strategy for the preparation of long-acting injectables. Aqueous suspensions are typically prepared by top-down approaches, e.g., wet bead media milling or high-pressure homogenization, containing the active pharmaceutical compound and surfactants and/or polymers for stabilization purposes. Currently, the screening of proper stabilizers and adequate stabilizer concentration during formulation investigations is based on a trial-and-error approach with variations in combinations, concentrations, and/or ratios. To obtain a more efficient methodology during formulation screening, the present study investigated the correlation between the surface activity of two different surfactants, i.e., poloxamer 188 and polysorbate 20, by drop profile tensiometry and Langmuir trough monolayer, and the obtained sizes of cinnarizine particles as a tool to predict the optimal surfactant concentration to prepare physical stable nano- and microsuspensions. The obtained results demonstrated that the molecular area determined as the area per surfactant molecule measured in the Langmuir trough combined with the specific surface area of the prepared suspensions could be used to predict the suitable concentration of the surfactant based upon short-term stress stability data. The results further showed that higher concentrations of poloxamer 188 were necessary to stabilize the suspensions when compared to the needed concentration of polysorbate 20. In addition, it was observed that there was a need for a slightly higher surfactant concentration when the suspensions were milled with the smallest bead size of 0.5 mm instead of larger sizes of bead (0.8 and 1.0 mm), which could not be accounted for by differences in specific surface area.

Current Formulation Strategies to Design Novel Carriers for Targeted Drug Delivery and Management of Infectious Keratitis: A Comprehensive Review on the Present State of the Art

Objective: Infectious keratitis is a pernicious disease that affects the anterior segment of the eye and is one the leading causes of blindness worldwide. This disease may cause severe visual impairment or permanent vision damage if left untreated. Discussion: No doubt there are many conventional drug delivery systems to treat ocular keratitis, yet it is the fifth leading cause of blindness globally. This is the result of the eye's complex anatomy and barrier system, which restricts the total ocular contact time of the conventional formulations resulting in underdosing. The widely used traditional formulations to treat keratitis, like antibiotic eye drops and ointments, are rendered useless due to less ocular contact time and low therapeutic drug levels at the target ocular site. The main requirement of the present time is to develop novel drug delivery-backed stratagems to overcome the shortcomings of conventional formulations, which will reduce the morbidity associated with infectious keratitis and improve clinical outcomes. It is worth mentioning that there are documented incidents of Herpetic keratitis of the cornea followed by COVID-19 infection and vaccination. Conclusion: This paper is a rigorous review of all the novel drug delivery strategies to combat ocular keratitis. These future drug delivery strategies will pave the way for the present time researcher and formulation chemists to develop multi-dimensional novel formulations that are safe, patient-compliant, and surpass the ocular barriers to maintain therapeutic drug levels in ocular tissues.

Sonication-Assisted Self-Assembled Resveratrol Nanoparticles with Enhanced Antiviral and Anti-inflammatory Activity against Respiratory Syncytial Virus-Induced Pneumonia.

Respiratory syncytial virus (RSV)-induced viral pneumonia in children is common worldwide. Its high occurrence and lack of an effective vaccine make it a leading cause of death in children. Severe RSV infection can trigger uncontrolled inflammatory responses in patients, so the development of small molecule drugs with the dual function of "direct antivirus" and "inflammatory response regulation" is welcome. Resveratrol (Res) has been reported to have antiviral and anti-inflammatory pharmacological effects, but its application is limited because of its poor water solubility and oral bioavailability. Based on small-molecule nanotechnology, we developed a sonication-assisted self-assembly method for preparing insoluble Res into highly soluble resveratrol nanoparticles (Res NPs). The obtained Res NPs exhibited a higher water solubility and a faster dissolution rate, which was more conducive to the effectiveness of Res in addressing RSV-induced viral pneumonia. In vitro studies had shown that Res NPs played an antiviral role by inhibiting RSV replication and reducing the production of pro-inflammatory cytokines. Nebulized inhalation administration of Res NPs prolonged the drug's residence time in the lungs, which appears to increase the accumulation and effectiveness of Res NPs. Additionally, in vivo studies had demonstrated significant benefits of Res NPs in inhibiting RSV viral load and improving the pulmonary microenvironment in RSV-infected mice. Both antiviral and anti-inflammatory experiments had confirmed that the pharmacological activity of Res NPs is superior to that of Res. This suggested that nanosizing Res was an effective way to enhance the original pharmacological activity of Res and also offered a new formulation strategy for treating viral pneumonia.

91 Awardee Talk: Using respiration calorimetry to estimate energy balance to estimate energy balance and methane emissions

Abstract Understanding relationships between chemical components of the diet and methane production will allow nutritionists to develop formulation strategies to decrease methane emissions. Diets that produce acetate liberate hydrogen that can be used by methanogenic archaea to produce methane. Propionate is a hydrogen sink and diets that lead to increased propionate production decrease acetate and methane production. The objective was to evaluate relationships between methane emissions and dietary chemical components and feed intake using published databases and make diet formulation recommendations that could be used to decrease methane production in finishing beef cattle. A total of 263 treatment mean observations from respiration calorimetry studies with beef cattle and dairy steers and heifers were used to evaluate relationships between methane emissions, dietary chemical components, and feed intake. Among the chemical components evaluated, dietary neutral detergent fiber and starch were strongly related to methane yield. The relationship between dietary ether extract and methane yield was variable and there was no relationship between dietary crude protein concentration and methane yield. Additionally, the ratio of metabolizable energy relative to gross energy intake had a strong relationship to methane yield. Formulation strategies to increase dietary starch and decrease dietary neutral detergent fiber should allow the feedlot industry to decrease enteric methane production.

Towards more sustainable, nutritious, and affordable plant‐based milk alternatives: A critical review

AbstractThe consumer market has seen a surge in various types of plant‐based milk alternatives (PBMAs), driven by factors such as sustainability, ethics, and the availability of diverse options. However, the global adoption of PBMAs is still hindered by potential nutritional concerns and cost‐ineffectiveness. It is therefore paramount to understand the status and challenges of these alternatives, encompassing production, stabilization strategies, nutrition and health, digestion, and environmental impacts. This review provides a comprehensive examination of these aspects. We begin by scrutinizing the production processes and formulation strategies of PBMAs, followed by an exploration of fundamental stabilization aspects, including homogenization, emulsification, thickening, and quantitative measurements of stabilization. Additionally, we discuss their nutrition facts and potential health benefits, as well as potential differences in the digestion of nutrients from PBMAs. Importantly, their challenges and future directions are discussed individually, highlighting the need for a fundamental understanding and effective food technologies to develop sustainable, nutritious, tasty, and affordable PBMAs. For example, several critical aspects involve maximizing the use of plant materials (e.g., proteins, fibers, and bioactive compounds) and using reliable and unified life cycle analyses to guide the development. This review offers valuable insights for researchers, food technologists, and consumers seeking to navigate and develop the landscape of PBMAs effectively.

Hot Melt Extruded High-Dose Amorphous Solid Dispersions Containing Lumefantrine and Soluplus

Over the last 15 years, a small number of paediatric artemisinin-based combination therapy products have been marketed. These included Riamet® and Coartem® dispersible tablets, a combination of artemether and lumefantrine, co-developed by the Medicines for Malaria Venture and Novartis. Disappointingly, patient compliance, requirement for high-fat meal, and sporadic drug dissolution behaviours following administration still result in considerable challenges for these products. The first and foremost barrier that needs addressed for successful delivery of the artemether/lumefantrine combination is the poor solubility of lumefantrine within the gastrointestinal fluids. In this work, amorphous solid dispersions of lumefantrine within Soluplus®-based matrices have been manufactured using hot melt extrusion as a potential formulation strategy to achieve enhanced dissolution and apparent solubility. The drug loading capacity of Soluplus® to accommodate amorphous lumefantrine, whilst ensuring improved in-vitro dissolution performance, was investigated. The extrusion process employed a variety of processing parameters, including various temperature profiles and different production scales. The influence of variation in extrusion conditions upon the physical stability of manufactured amorphous solid dispersions was also examined. This allowed for a greater understanding of the role of extrusion processing conditions on the performance of supersaturated amorphous solid dispersions during dissolution and storage. This may allow for the design and manufacture of drug enabled formulations with lower drug dosing and thus a lower risk of adverse effects.

Novel pectin-carboxymethylcellulose-based double-layered mucin/chitosan microcomposites successfully protect the next-generation probiotic Akkermansia muciniphila through simulated gastrointestinal transit and alter microbial communities within colonic ex vivo bioreactors

The rapid acceleration of microbiome research has identified many potential Next Generation Probiotics (NGPs). Conventional formulation processing methods are non-compatible, leading to reduced viability and unconfirmed incorporation into intestinal microbial communities; consequently, demand for more bespoke formulation strategies of such NGPs is apparent. In this study, Akkermansia muciniphila (A.muciniphila) as a candidate NGP was investigated for its growth and metabolism properties, based on which a novel microcomposite-based oral formulation was formed. Initially, a chitosan-based microcomposite was coated with mucin to establish a surface culture of A.muciniphila. This was followed by ‘double encapsulation’ with pectin (PEC) using a novel Entrapment Deposition by Prilling method to create core–shell double-encapsulated microcapsules. The formulation of A.muciniphila was verified to require no oxygen-restriction properties, and additionally, biopolymers were selected, including carboxymethylcellulose (CMC), that support and enhance its growth; consequently, a high viability (6 log CFU/g) of A.muciniphila microencapsulated in PEC-CMC double-encapsulates was obtained. Subsequently, the high stability of the PEC-CMC double-encapsulates was verified in simulated gastric fluid, successfully protecting and then releasing the A.muciniphila under intestinal conditions. Finally, employing a model of gastrointestinal transit and faecal-inoculated colonic bioreactors, significant alterations in microbial communities following administration and successful establishment of A.muciniphila were demonstrated.