Lipid-based Formulations Research Articles

Development of polymer-encapsulated microparticles of a lipophilic API-IL and its lipid based formulations for enhanced solubilisation.

Active Pharmaceutical Ingredient-Ionic liquids (API-ILs) have the potential to improve the bioavailability of BCS Class IV Drugs. However, the problematic physical handling properties of room temperature API-ILs have impaired clinical and commercial exploitation to date. Lipid-based formulations (LBFs) are used to improve the absorption of drugs with limited bioavailability. Nonetheless, LBFs face limitations such as low drug loading capacity and sub-par physical stability. A platform for transforming API-ILs into solid forms at high loadings via spray encapsulation with polymers has been developed and previously demonstrated for hydrophilic API-ILs. The current work demonstrates that this platform technology can be applied to a lipophilic API-IL of the BCS Class IV API, chlorpromazine, and to multi-component solutions comprising API-IL and a LBF. Furthermore, solidification of a type IIIB, liquid LBF was achieved via spray encapsulation with cellulose- and methacrylate- based polymers for the first time. The spray-encapsulated formulations had excellent physical handling properties, and successfully eluted the API-IL in aqueous media. The chlorpromazine release profiles from the API-IL, the API-IL containing LBF, and the solidified formulations, were evaluated in vitro using phosphate buffer (pH 6.8) and fasted state simulated intestinal fluid (FaSSIF). Spray-encapsulated formulations exhibited improved release profiles compared to the liquid formulations. Overall, these findings indicate that phase-separated, polymeric, solid formulations of liquid API forms represent a promising platform technology for developing oral solid dosage forms of poorly bioavailable drugs.

Nanoparticles Encapsulating Phosphatidylinositol Derivatives Promote Neuroprotection and Functional Improvement via a long-lasting activation of TRPML1 lysosomal channel in Preclinical Models of ALS.

Amyotrophic lateral sclerosis (ALS) is a progressive neurodegenerative disease currently incurable, in which motor neuron degeneration leads to voluntary skeletal muscle atrophy. Molecularly, ALS is characterized by protein aggregation, synaptic and organellar dysfunction, and Ca2+ dyshomeostasis. Of interest, autophagy dysfunction is emerging as one of the main putative targets of ALS therapy. A tune regulation of this cleansing process is affordable by a proper stimulation of TRPML1, one of the main lysosomal channels. However, TRPML1 activation by PI(3,5)P2 has low open probability to remain in an active conformation. To overcome this drawback we developed a lipid-based formulation of PI(3,5)P2 whose putative therapeutic potential has been tested in in vitro and in vivo ALS models. Pharmacodynamic properties of PI(3,5)P2 lipid-based formulations (F1 and F2) on TRPML1 activity have been characterized by means of patch-clamp electrophysiology and Fura-2AM video-imaging in motor neuronal cells. Once selected for the ability to stabilize TRPML1 activity, the most effective preparation F1 was studied in vivo to measure neuromuscular function and survival of SOD1G93A ALS mice, thereby establishing its therapeutic profile. Key Results F1, but not PI(3,5)P2 alone, stabilized the open state of the lysosomal channel TRPML1 and increased the persistence of intracellular calcium concentration ([Ca2+]i). Then, F1 was effective in delaying motor neuron loss, improving innervated endplants and muscle performance in SOD1G93A mice, extending overall lifespan by an average of 10 days. Of note F1 prevented gliosis and autophagy dysfunction in ALS mice by restoring PI(3,5)P2 level. Our novel self-assembling lipidic formulation for PI(3,5)P2 delivery exerts a neuroprotective effect in preclinical models of ALS mainly regulating dysfunctional autophagy through TRPML1 activity stabilization.

Development and validation of a stability-indicating HPLC method for assay of tonabersat in pharmaceutical formulations

A stability-indicating reversed-phase high-performance liquid chromatography (RP-HPLC) method was developed to assay tonabersat and assess its stability in pharmaceutical formulations. Chromatographic separation was achieved using a Kinetex® C18 column (2.6 µm, 150 x 3 mm, 100 Å) at 50 °C, with a 20 µL injection volume. A linear gradient of acetonitrile in water (5 – 33.5 %) was applied for 1 min, followed by a gradual increase to 100 % over 26 min at a flow rate of 0.5 mL/min. Tonabersat and its degradation products were detected at 275 nm and 210 nm, respectively. The optimized method was used to evaluate the stability of tonabersat in lipid-based pharmaceutical formulations at 5 ± 3 °C, 25 ± 2°C/60 ± 5 % RH, and 40 ± 2 °C/75 ± 5 % RH over 3 months. The method was validated as per ICH guidelines and demonstrated linearity in the range of 5 – 200 µg/mL (R2 = 0.99994) with good accuracy (98.25 – 101.58 % recovery) and precision (% RSD < 2.5 %). The limits of detection and quantitation were 0.8 µg/mL and 5 µg/mL, respectively. Forced degradation studies showed significant degradation on exposure to alkaline (90.33 ± 0.80 %), acidic (70.60 ± 1.57 %), and oxidative stress (33.95 ± 0.69 %) at 70 °C, but no degradation was observed on exposure to thermal or photolytic stress. No chemical degradation was observed in either formulation on storage. Thus, the method was sensitive, specific, and suitable for stability testing of tonabersat in pharmaceutical formulations.

Quality by Design Approach for the Development of Cariprazine Hydrochloride Loaded Lipid-Based Formulation for Brain Delivery via Intranasal Route.

Cariprazine (CPZ) is a third-generation antipsychotic medication that has been approved for treating schizophrenia. This study aimed to develop a cariprazine-loaded nanostructured lipid carrier (CPZ-NLCs) to prevent first-pass metabolism and improve bioavailability and site-specific delivery from the nose to the brain. The CPZ-NLCs were prepared using melt emulsification. The formulation was optimized using the Box-Behnken design (BBD); where the influence of independent variables on critical quality attributes, such as particle size and entrapment efficiency, was studied. The optimized batch (F6) had a particle size of 173.3 ± 0.6 nm and an entrapment efficiency of 96.1 ± 0.57%, respectively. The in vitro release showed >96% release of CPZ from NLC within 30 min. The optimized formulation's ex vivo studies revealed significantly increased CPZ permeability (>75%) in sheep nasal mucosa compared to the CPZ suspension (~26%). The ciliotoxicity study of the nasal mucosa revealed that the CPZ-NLC formulation did not affect the nasal epithelium. The intranasal administration of the formulation achieved 76.14±6.23 μg/ml concentration in the brain which was significantly higher than the oral CPZ suspension administration (30.46±7.24 μg/ml). The developed formulation was stable for 3 months. The study concluded that the developed CPZ-NLC could significantly improve the bioavailability with quick delivery to the brain.

Inhalable Dry Powders for Lung mRNA Delivery.

Despite great promise, application of mRNA therapeutics in the lung has proven challenging. Many groups have reported success instilling liquid mRNA formulations in animal models, but direct intratracheal administration of large liquid quantities to the human lung presents significant safety and distribution concerns. To accomplish safe and effective mRNA delivery to the lung, formulations must be prepared for dosing via inhalation. An inhaled mRNA delivery system for the lung must be both robust enough to survive inhalation conditions and potent enough to deliver mRNA upon reaching the lung. In this work dry powder lipid nanoparticle formulations are developed, using spray-freeze-drying, to produce stable, biologically active, inhalable dry powders for mRNA delivery. The final powders have suitable aerosolization properties, with mean mass aerodynamic diameter (MMAD) of 3-4 microns, and fine particle fraction (FPF) ≈40%, allowing for efficient mRNA delivery to the deep lung following inhalation. Importantly, the formulations developed here are suitable for use with different ionizable lipids. Four different ionizable lipid-based formulations are evaluated as powders, and all exhibit in vivo pulmonary mRNA delivery equal to that of instilled liquid formulations. These results lay promising groundwork for the eventual development of an inhalable mRNA dry powder therapeutic.

Lipid-Based Formulation of Baricitinib for the Topical Treatment of Psoriasis

Background: Baricitinib, commonly used for autoimmune diseases, is typically administered orally, which can lead to systemic adverse effects. A topical formulation could potentially offer localized therapeutic effects while minimizing these side effects. Objectives: This study focuses on developing a lipid-based topical formulation of baricitinib (BCT-OS) for treating psoriasis. Methods: The optimized formulation was then assessed for physical, chemical, and biopharmaceutical characterization. Furthermore, the anti-inflammatory efficacy of the formulation was tested in a model of psoriasis induced by imiquimod in mice, and its tolerance was determined by the evaluation of biomechanical skin properties and an inflammation test model induced by xylol in mice. Results: BCT-OS presented appropriate characteristics for skin administration in terms of pH, rheology, extensibility, and stability. The formulation also demonstrated a notable reduction in skin inflammation in the mouse model, and high tolerability without affecting the skin integrity. Conclusions: BCT-OS shows promise as an alternative treatment for psoriasis, offering localized therapeutic benefits with a potentially improved safety profile compared to systemic administration.

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.

Product development and characterization of a lipid-based Ayurvedic polyherbal formulation: Kalyanaka Ghrita

BackgroundKalyanaka Ghrita (KG) is polyherbal oleaginous medicament consisting of extracts from twenty-eight different plants, indicated for management of psychosomatic disorders like Unmada (Schizophrenia), Apasmara (Epilepsy) and numerous other ailments. ObjectiveTo develop and validate standard manufacturing procedure of KG by following Ayurvedic principles in three batches to ensure process uniformity and standards. Materials and methodsThree batches of KG were prepared by adopting principles of Ashtanga Hrudya and Ayurvedic Formulary of India to ensure consistency in manufacturing process. Observations during process such as temperature, duration were recorded. KG was subjected to chief desired characteristics, organoleptic (color, odour, taste, texture, touch), physicochemical (acid value, peroxide value, iodine value, saponification value, loss on drying, refractive index, specific gravity, mineral oil, rancidity test, viscosity) as per pharmacopeial standard. Chromatographic screening and fingerprinting of KG were conducted through GCMS whereas quantification of curcumin and chebulagic acid biomarkers were assessed through HPLC. ResultsAverage yield of KG was 83.41%, with average intermittent heating duration of 20.35 h subsequently divided into three days. Temperature throughout preparation ranged from 66 °C to 101 °C. KG was pale olive in colour, exhibiting pleasant taste, characteristic smell, and soft texture. Organoleptic and physicochemical characters were comparable for three batches of KG while safety parameters were found within permissible limits. ConclusionPharmaceutical standardization of Kalyanaka Ghrita is necessary for establishing biological and chemical profile of formulations. Present study recommends use of coarse powdered ingredients for optimal yield during pharmaceutical process, and heating up to Madhyama Paka stage calibrated over three days with average temperature of 85 °C. The data obtained from this study may contribute to future research and development activities, serving as a basis for manufacturing standards of KG.

Exploring lipids: A comprehensive review on their utilization in the formulation of liposomes, phytosomes, and ethosomes for advanced drug delivery systems"

This comprehensive review explores the diverse applications of lipids in the formulation of advanced drug delivery systems, specifically focusing on liposomes, phytosomes, and ethosomes. Lipids, crucial components in these formulations, play a pivotal role in enhancing drug solubility, stability, and bioavailability. The review systematically examines the latest advancements in lipid-based delivery systems, shedding light on their unique characteristics and applications. In the realm of liposomes, the study delves into various lipid compositions, highlighting their influence on liposomal structure and function. Additionally, the review explores the integration of phytosomes, which involve the complexation of drugs with plant-derived phospholipids, showcasing their potential to improve therapeutic efficacy. Ethosomes, lipid vesicles containing high concentrations of ethanol, are also extensively discussed, emphasizing their ability to enhance transdermal drug delivery. Critical analyses of recent research findings, including the impact of lipid selection on vesicle stability, drug release kinetics, and pharmacokinetics, are presented. The review further examines the challenges associated with lipid-based formulations, providing insights into potential avenues for future research and development. By synthesizing current knowledge, this review serves as a valuable resource for researchers, clinicians, and pharmaceutical scientists seeking a comprehensive understanding of the role of lipids in optimizing liposomal, phytosomal, and ethosomal drug delivery systems.

Antimalarial activity of caffeine, orally administered with a lipid-based formulation in a Murine model

Antimalarial activity of caffeine, orally administered with a lipid-based formulation in a Murine model

Novel Approaches and Applications of Nanotechnology in the Delivery of Topical Drugs for Psoriasis via Nanocarriers

Psoriasis is a non-contagious, continuing, auto-immune disease that mostly affects the skin, and about 2%-3% of the world's population suffers from it. In this review article, the primary focus is on the strategies involved in conventional therapies and the latest advances that have been recorded in metallic nano, polymer-based, and lipid-based formulations in the spectrum of anti-psoriatic drugs. Liposomes, ethosomes, solid lipid nanoparticles, micelles, and dendrimers are only some of the nanocarrier systems that have been extensively researched in relation to their potential use in nano formulations. This study incorporates patent applications that illustrate the nanoparticle's function in treating psoriasis. Hence, on the basis of an extensive literature survey, it is concluded that nano-formulations are a promising medium to treat a disease like psoriasis as they offer enhanced penetration, target-specific delivery, and improved efficacy. When applied to the study of biological systems and the development of novel medical technologies, nanobiotechnology offers potentially promising possibilities for the efficient use of nanoscale materials and processes. In this approach, nanotechnology and biotechnology are combined in order to develop nanoscale devices, materials, and systems that can be used for the diagnosis, treatment, and prevention of psoriasis. The future of the therapeutic effect of antipsoriatic drugs is dependent on both the benefits they have the ability to bring and the progress being made in the mass production of these carriers. Researching novel carrier systems or combination therapies is essential, but so is working to scale up existing technologies so they may be commercialised and used to benefit society at large.

Personalization of lipid-based oral dosage forms via filament-based 3D-printing

While filament-based 3D-printing (3DP) is the most utilized 3DP technology in the pharmaceutical field, it has not been demonstrated for processing of drug-loaded lipid-based formulations. This work exploits hexa-glycerol ester of palmitic acid (Pg6-C16-P) as an advanced lipid material, loaded with felodipine as a poorly soluble model drug, for fabricating novel oral solid dosage forms (OSDFs) via filament-based 3D-printing. After material melt-blending, the formulation was extruded using the liquid feeding approach to obtain a mechanically manageable, and hence 3D-printable, drug-loaded lipid filament. The fabrication of geometries with variable infill densities was demonstrated. The extent of infill density was found to significantly impact the optimal printing parameters required to achieve the desired shape. The solid-state analysis confirmed the amorphous state of felodipine after 3DP. The release rate of the drug was studied via in vitro dissolution test and showed to be tunable based on the tablet geometry. It was also possible to tailor the design of the dosage form to perform similarly to a commercial product. The formulation was evidenced as safe via in vitro toxicity studies with improved felodipine solubility. This study establishes filament-based 3DP as an alternative platform viable for fabricating advanced lipid-based OSDFs, and concurrently, promotes Pg6-C16-P as a promising and high performing 3DP lipid material for drug delivery.

Thermally-Induced Supersaturation Approach for Optimizing Drug Loading and Biopharmaceutical Properties of Supersaturated Lipid-Based Formulations: Case Studies with Ibrutinib and Enzalutamide.

Lipid-based formulations (LbFs) have demonstrated success in pharmaceutical applications; however, challenges persist in dissolving entire doses of the drug into defined liquid volumes. In this study, the temperature-induced supersaturation method was employed in LbF to address drug loading and pill burden issues. Supersaturated LbFs (super-LbF) were prepared using the temperature-induced supersaturation method, where the drug load is above its equilibrium solubility. Further, the influence of the drug's physicochemical and thermal characteristics on drug loading and their relevance with an apparent degree of supersaturation (aDS) was studied using two model drugs, ibrutinib and enzalutamide. All the prepared LbFs were evaluated in terms of physical stability, dispersion, and solubilization capacity, as well as pharmacokinetic assessments. Drug re-crystallization was observed in the lipid solution on long-term storage at higher aDS values of 2-2.5. Furthermore, high-throughput lipolysis studies demonstrated a significant decrease in drug concentration across all LbFs (regardless of drug loading) due to a decline in the formulation solvation capacity and subsequent generation of in-situ supersaturation. Further, the in vivo results demonstrated comparable pharmacokinetic parameters between conventional LbF and super-LbF. The short duration of the thermodynamic metastable state limits the potential absorption benefits. However, super-LbFs of Ibr and Enz showed superior profiles, with 1.7-fold and 5.2-fold increased drug exposure compared to their respective crystalline suspensions. In summary, this study emphasizes the potential of temperature-induced supersaturation in LbF for enhancing drug loading and highlights the intricate interplay between drug properties, formulation characteristics, and in vivo performance.

Anticancer drug delivery: Investigating the impacts of viscosity on lipid-based formulations for pulmonary targeting

Pulmonary drug delivery via aerosolization is a non-intrusive method for achieving localized and systemic effects. The aim of this study was to establish the impact of viscosity as a novel aspect (i.e., low, medium and high) using various lipid-based formulations (including liposomes (F1-F3), transfersomes (F4-F6), micelles (F7-F9) and nanostructured lipid carriers (NLCs; F10-F12)) as well as to investigate their impact on in-vitro nebulization performance using Trans-resveratrol (TRES) as a model anticancer drug. Based on the physicochemical properties, micelles (F7-F9) elicited the smallest particle size (12–174 nm); additionally, all formulations tested exhibited high entrapment efficiency (>89 %). Through measurement using capillary viscometers, NLC formulations exhibited the highest viscosity (3.35–10.04 m2/sec). Upon using a rotational rheometer, formulations exhibited shear-thinning (non-Newtonian) behaviour. Air jet and vibrating mesh nebulizers were subsequently employed to assess nebulization performance using an in-vitro model. Higher viscosity formulations elicited a prolonged nebulization time. The vibrating mesh nebulizer exhibited significantly higher emitted dose (ED), fine particle fraction (FPF) and fine particle dose (FPD) (up to 97 %, 90 % and 64 µg). Moreover, the in-vitro release of TRES was higher at pH 5, demonstrating an alignment of the release profile with the Korsmeyer-Peppas model. Thus, formulations with higher viscosity paired with a vibrating mesh nebulizer were an ideal combination for delivering and targeting peripheral lungs.

Lipid-based nanocarriers mediated Axitinib retinal delivery after topical instillation: Formulations setting up and in vivo evidence

Axitinib (AXB) is a multi-receptor tyrosine kinase inhibitor molecule. It acts by blocking the receptors for vascular endothelial growth factor (VEGFR) and platelet-derived growth factor (PDGFR), which are responsible for the development of neovascularization. To date, intravitreal injections of anti-VEGF have become the first-line medical treatment for diabetic macular oedema, a degeneration of diabetic retinopathy. Despite the efficacy of intravitreal injections, the complications of this type of administration are manifold. Our study aimed to design a nanotechnological formulation capable of delivering AXB to the retinal area after topical administration. Two different lipid-based formulations, namely solid lipid nanoparticles (SLN) and nanostructured lipid nanocarriers (NLC) were developed through a design of experiment (DoE) approach. The formulations possessed a mean particle size below 200 nm, low PDI values and a high drug encapsulation efficiency, thus designating them as suitable for ocular administration. Stability studies were performed at different storage conditions according to ICH guidelines. Strategies to improve AXB concentration in the retinal target were finally developed, such as using cationic lipids and increasing AXB loading in the nanocarriers. The in vivo PK studies indicated that cationic NLC loaded with AXB at 4 mM were the most efficient in delivering the drug to the retina, proposing them as a potential topical treatment for DR.

Optimization of Lipid-Based Nanoparticles Formulation Loaded with Biological Product Using A Novel Design Vortex Tube Reactor via Flow Chemistry.

Lipid-based nanoparticles (LNPs) is increasingly recognized for their potential in drug delivery, offering protection to hydrophobic drugs from degradation. Industrial synthesis of LNPs, exemplified by Pfizer-BioNTech and Moderna mRNA vaccines, utilizes flow chemistry or microfluidics, showcasing its scalability. This study explores the utilization of a novel design reactor, the vortex tube reactor, within flow chemistry for LNPs synthesis, aiming to optimize its conditions and compare them with batch synthesis. LNPs were synthesized using the vortex tube reactor, incorporating bovine serum albumin (BSA) as a model drug in the aqueous phase, alongside 1.2-dipalmitoyl-sn-glycero-3-phosphocholine (DPPC) and cholesterol in the organic phase. Design of experiments (DoE), specifically Box-Behnken design, was employed to optimize parameters, including X1: the flow rate ratio (10-100 mL/min), X2: the aqueous-to-organic volumetric ratio (1:1-10:1), and X3: the number of reactor units (1-5 units). Responses evaluated encompassed physical properties and productivity. Optimized conditions were determined by minimizing particle size (Y1), polydispersity index (Y2), and zeta potential (Y3), while maximizing entrapment efficiency (Y4), drug loading (Y5), and productivity (Y5). Results indicated that optimal conditions were achieved at X1 of 100 mL/min, X2 of 5.278, and X3 of 1 unit. LNPs synthesized under these conditions exhibited favorable physical properties and productivity, with uniformity maintained across batches. The vortex tube reactor demonstrated superiority over batch synthesis, yielding smaller particles (166.23 ± 0.98 nm), more uniform nanoparticles (PDI 0.17 ± 0.01), and higher entrapment (67.75 ± 1.55%) and loading capacities (36.39 ± 0.83%), indicative of enhanced productivity (313.4 ± 12.88 mg/min). This study elucidates the potential of flow chemistry, particularly utilizing the vortex tube reactor, for large-scale LNPs formulation, offering insights into parameter relationships and advancing nanoparticle synthesis for drug delivery applications.

Antitumoral activity of a CDK12 inhibitor in colorectal cancer through a liposomal formulation

Colorectal cancer (CRC) is the third most common cancer worldwide. Recent experiments suggest that CDK12 can be a good therapeutic target in CRC, and therefore, novel inhibitors targeting this protein are currently in preclinical development. Lipid-based formulations of chemical entities have demonstrated the ability to enhance activity while improving the safety profile. In the present work, we explore the antitumor activity of a new CDK12 inhibitor (CDK12-IN-E9, CDK12i) and its lipid-based formulation (LP-CDK12i) in CRC models, to increase efficacy. SW620, SW480 and HCT116 CRC cell lines were used to evaluate the inhibitor and the liposomal formulation using MTT proliferation assay, 3D invasion cultures, flow cytometry, Western blotting and immunofluorescence experiments. Free-cholesterol liposomal formulations of CDK12i (LP-CDK12i) were obtained by solvent injection method and fully characterized by size, shape, polydispersity, encapsulation efficiency, and release profile and stability assessments. LP-CDK12i induced a higher antiproliferative effect compared with CDK12i as a free agent. The IC50 value was lower across all cell lines tested, leading to a reduction in cell proliferation and the formation of 3D structures. Evaluation of apoptosis revealed an increase in cell death, while biochemical studies demonstrated modifications of apoptosis and DNA damage components. In conclusion, we confirm the role of targeting CDK12 for the treatment of CRC and describe, for the first time, a liposomal formulation of a CDK12i with higher antiproliferative activity compared with the free compound.

Efficacy and Safety of Miebo® (Perfluorohexyloctane Ophthalmic Solution) in Treating Dry Eye Disease - a narrative review

Introduction: Dry eye disease (DED) is a prevalent and debilitating ocular condition characterized by discomfort, visual disturbances, and tear film instability. Recent therapeutic developments have introduced perfluorohexyloctane ophthalmic solution (Miebo®) as a potential treatment for DED, particularly in patients with meibomian gland dysfunction (MGD). Aim of the Study: This narrative review aims to evaluate the efficacy and safety of Miebo® in treating DED based on current clinical evidence. Materials and Methods: A comprehensive literature search was conducted in PubMed, Embase, and Cochrane Library databases up to May 2024 resulting in the identification of 9 studies. The review included randomized controlled trials, prospective cohort studies, and systematic reviews that focused on the use of Miebo® for DED. Data on efficacy in improving tear film stability and symptom relief, as well as safety profiles, were extracted and analyzed. Results: The evidence indicates that Miebo® significantly enhances tear film stability and alleviates symptoms of DED, with pronounced benefits observed in patients with MGD. Comparative studies demonstrate that Miebo® is more effective than conventional treatments, such as artificial tears and lipid-based formulations. Safety assessments reveal minimal ocular surface discomfort and no significant systemic adverse events associated with Miebo® use. Conclusion: Miebo® shows substantial efficacy and a favorable safety profile in managing DED, making it a valuable therapeutic option, particularly for patients who do not respond to traditional therapies. However, further research is needed to confirm its long-term effectiveness and safety.

Benefits of combining supersaturating and solubilizing formulations – Is two better than one?

A variety of enabling formulations has been developed to address poor oral drug absorption caused by insufficient dissolution in the gastrointestinal tract. As the in vivo performance of these formulations is a result of a complex interplay between dissolution, digestion and permeation, development of suitable in vitro assays that captures these phenomena are called for. The enabling-absorption (ENA) device, consisting of a donor and receiver chamber separated by a semipermeable membrane, has successfully been used to study the performance of lipid-based formulations. In this work, the ENA device was prepared with two different setups (a Caco-2 cell monolayer and an artificial lipid membrane) to study the performance of a lipid-based formulation (LBF), an amorphous solid dispersion (ASD) and the potential benefit of combining the two formulation strategies. An in vivo pharmacokinetic study in rats was performed to evaluate the in vitro-in vivo correlation. In the ENA, high drug concentrations in the donor chamber did not translate to a high mass transfer, which was particularly evident for the ASD as compared to the LBF. The solubility of the polymer used in the ASD was strongly affected by pH-shifts in vitro, and the ph_dependence resulted in poor in vivo performance of the formulation. The dissolution was however increased in vitro when the ASD was combined with a blank lipid-based formulation. This beneficial effect was also observed in vivo, where the drug exposure of the ASD increased significantly when the ASD was co-administered with the blank LBF. To conclude, the in vitro model managed to capture solubility limitations and strategies to overcome these for one of the formulations studied. The correlation between the in vivo exposure of the drug exposure and AUC in the ENA was good for the non pH-sensitive formulations. The deconvoluted pharmacokinetic data indicated that the receiver chamber was a better predictor for the in vivo performance of the drug, however both chambers provided valuable insights to the observed outcome in vivo. This shows that the advanced in vitro setting used herein successfully could explain absorption differences of highly complex formulations.

Luxurious Locks: Harnessing the Power of Lipids for Transformative Hair Care Solutions

Abstract: The hair is a distinguishing feature of animals that has several functions, such as providing warmth, providing protection, facilitating sweating and pheromone evaporation, providing sensory stimulation, and, in certain situations, acting as color-based camouflage. Hair grooming and styling have progressed significantly over the years, and modern hair treatments primarily focus on enhancing hair quality. However, standard active ingredients in formulations display suboptimal performance, and some may present toxicity issues, demanding a stronger formulation design that is appropriate for performance and safety. The need for natural ingredients, such as macromolecules and biomolecules sourced from plants, animals, and marine environments, is increasing among consumers. The favorable benefits induced by including lipid-rich components in Personal Care Products (PCP) formulations are regarded as valuable elements. A lipid-based preparation is specifically employed for innovative medicine-targeted distribution of bioactive substances among all medication administration strategies. The distribution of LBDDS transdermally and topically is exciting since the lipid bilayer might enter the uppermost layer of skin with ease and release medicine in a regulated way. It offers benefits in terms of stability, bioacceptability, and biodegradability, as well as receptor-mediated fast absorption by the particular site. Various lipid-based formulations for hair care therapy have been created, showing some improvement in hair care. This review focuses on several lipid-based formulations for hair care therapy, including their thorough mechanism of action, efficacy on hair care, patents, obstacles, and future prospects, along with the challenges and future prospects in the hair care industry