Vesicular Systems Research Articles

Innovative approaches in characterizing and developing methods for lipoidal vesicular drug delivery systems

Lipoidal vesicular systems, including liposomes, ethosomes, and transferosomes, represent a significant advancement in targeted drug delivery, offering enhanced bioavailability, controlled release, and specific targeting capabilities. This review discusses the types of lipoidal vesicular systems, their methods of characterization, method development, applications, advantages, challenges, and future perspectives. These systems have shown immense potential in diverse therapeutic areas, including cancer therapy, infectious diseases, gene therapy, and transdermal drug delivery. Despite the challenges in stability, scalability, and targeting, ongoing research and technological advancements promise to expand their applications and improve therapeutic outcomes.

Assessment of Brazil's vesicular syndrome surveillance system: Profile of notifications and performance of the official veterinary service

Foot-and-mouth disease (FMD) is an ailment that causes serious damage to the productive chain, and its control through vaccination is of utmost importance for its eradication. Brazil initiated the National Foot-and-Mouth Disease Surveillance Program (PNEFA) with the aim of making the country FMD-free by 2026. As part of the program, notifications of vesicular lesions became mandatory for the Official Veterinary Service (OVS), which is responsible for verifying them. Due to its size, border areas with countries that do not have FMD-free status pose a risk to Brazil and require greater attention. This study described the profile of notifications of suspected outbreaks of vesicular syndrome in Brazil and analyzed the performance of the surveillance system. The results showed 7134 registered notifications of suspected vesicular syndrome outbreaks from 2018 to 2022, with 2022 having the highest number (n = 2343 or 32.85 %). The species that generated the most notifications were swine (90.99 %), cattle and buffaloes (7.54 %), goats and sheep (1.44 %), and others (0.03 %). The sources of notification were "Veterinary medicine professionals" (61.82 %), "Owners or employees" (13.66 %), "Third parties" (8.90 %), "OVS" (7.20 %), and "others" (2.66 %). 41.69 % of notifications originated from non-border municipalities, and 58.32 % from border areas. Only the state of Paraná account for 51.73 % of the total notifications. This state also accounted for 66.70 % of the 32.47 % of notifications with a final diagnosis of "absence of clinically compatible signs or susceptible animals", indicating a certain lack of knowledge in the area, leading to unnecessary notifications and system overload. The performance of the OVS was evaluated based on the service response time from notification registration trough Logistic and Negative binomial regressions. A total of 27.83 % of notifications did not meet the Brazilian legally specified time, and the zone related to the state of Parana needs improvements in performance. The presence and peaks of Senecavirus A cases may have influenced an increased number of swine notifications and led to a decrease in OVS response time. The results demonstrate better performance of surveillance in border areas. Given the vast territory of Brazil, it is not expected that 100 % of responses occur within the legal timeframe, however, the performance of the surveillance system proved to be adequate, with 86 % complied to the legislation. The performance indicators could be used as a monitoring tool, along with indicators to demonstrate system overload. Continued education actions are crucial for strengthening PNEFA.

Exploring the Properties of Unilamellar Vesicle Bilayers Formed by Ionic Liquid Surfactants for Future Applications in Nanomedicine.

Two ionic liquids (ILs) with amphiphilic properties composed of 1-butyl-3-methylimidazolium dioctylsulfosuccinate (bmim-AOT) and 1-hexyl-3-methylimidazolium dioctylsulfosuccinate (hmim-AOT) form unilamellar vesicles spontaneously simply by dissolving the IL-like surfactant in water. These novel vesicles were characterized using two different and highly sensitive fluorescent probes: 6-propionyl-2-(dimethylaminonaphthalene) (PRODAN) and trans-4-[4-(dimethylamino)-styryl]-1-methylpyridinium iodide (HC). These fluorescent probes provide information about the physicochemical properties of the bilayer, such as micropolarity, microviscosity, and electron-donor capacity. In addition, the biocompatibility of these vesicles with the blood medium was evaluated, and their toxicity was determined using Dictyostelium discoideum amoebas. First, using PRODAN and HC, it was found that the bilayer composition and the chemical structure of the ions at the interface produced differences between both amphiphiles, making the vesicles different. Thus, the bilayer of hmim-AOT vesicles is less polar, more rigid, and has a lower electron-donor capacity than those made by bmim-AOT. Finally, the results obtained from the hemolysis studies and the growth behavior of unicellular amoebas, particularly utilizing the D. discoideum assay, showed that both vesicular systems do not produce toxic effects up to a concentration of 0.02 mg/mL. This elegant assay, devoid of animal usage, highlights the potential of these newly organized systems for the delivery of drugs and bioactive molecules of different polarities.

Nigella sativa Oil-loaded Ethanolic Vesicular Gel for Imiquimod-induced Plaque Psoriasis: Physicochemical Characterization, Rheological Studies, and In vivo Efficacy.

The therapeutic effect of NS oil in mild to moderate psoriasis is limited owing to low play load of thymoquinone ( < 15 %w/w), irritation, dripping, low viscosity and thus, less contact time on the lesions. This study aimed at developing and characterizing the ethanolic vesicular hydrogel system of Nigella sativa (NS) oil (NS EV hydrogel) for the enhancement of anti-psoriatic activity. The objective of this study was to develop NS EV hydrogel and evaluate its anti-psoriatic activity. The identification and quantification of TQ content in different NS seed extracts and marketed oil were measured by an HPTLC method using n-hexane and ethyl acetate as solvent systems. Preparation of ethanolic vesicles (EVs) was performed by solvent injection method, while its antipsoriatic activity was evaluated employing an Imiquad (IMQ)-induced plaque psoriasis animal model. A compact HPTLC band was obtained for TQ at an Rf value of 0.651. The calibration plot was linear in the range of 1-10 μg/spot, and the correlation coefficient of 0.990 was indicative of good linear dependence of peak area on concentration. From the different NS sources, the high TQ content was obtained in the marketed cold press oil, i.e., 1.45±0.08mg/ml. Out of various NS oilloaded EVs, the F6 formulation revealed the smallest particle size (278.1nm), with log-normal size distribution (0.459) and adequate entrapment efficiency. A non-uniform shape was observed in the transmission electron microscopy. The viscosity of F6 formulation hydrogel was 32.34 (Pa·s), which exhibited plastic behavior. In vivo, efficacy studies demonstrated decreased inflammation of the epidermis and dermis and a marked decrease in the levels of IL-17 by NS EV hydrogel compared to plain NS oil and standard drugs (Betamethasone and Dr. JRK Psorolin Oil). It may be concluded from the findings that NS-loaded EV gel was as good as betamethasone cream but more efficacious than the other treatments.

Molecular docking, molecular dynamics simulation, preparation, and characterization of naltrexone-phospholipid complex: A novel cargo with improved loading into multivesicular liposomes

Naltrexone hydrochloride (NTX), a water-soluble opioid receptor antagonist, is prescribed widely for opioid and alcohol dependence and pain reduction. However, the significant limitations of NTX are low lipophilicity and extensive first-pass metabolism. This study aimed to design and prepare a novel phospholipid complex of NTX and load it into multivesicular liposomes (MVLs). In silico studies, including molecular docking and molecular dynamics (MD) simulation, were performed to determine the interactions between NTX and phospholipid and evaluate their best molar ratio to prepare the complex, respectively. The NTX phospholipid complex was prepared by solvent evaporation technique and characterized by PXRD, SEM, FTIR, 1HNMR, solubility study, and n-octanol/water partition coefficient analyses. NTX-SPC complex-loaded MVLs (NTX-SPC-MVLs) were prepared by the double-emulsion method and characterized by encapsulation efficiency (EE)%, size, PXRD, FTIR, SEM, and release pattern. MD simulation reported the 1:1.5 M ratio of NTX to phospholipid as the best molar ratio. Complexation led to reduced water solubility and enhanced n-octanol/water partition coefficient. Loading of NTX-SPC complex into MVLs enhanced EE and extended the release duration in comparison to NTX MVLs. Thus, the NTX-SPC complex may be an appropriate system to enhance the physicochemical features of NTX and improve the EE in vesicular drug delivery systems like MVLs.

Polymeric liposomes of emtricitabine employing modified pullulan—an attempt to reduce associated hepatotoxicity

Emtricitabine (FTC) a BCS class I drug, is used for HIV prevention. The high solubility of the drug is the leading cause of severe hepatotoxicity and lactic acidosis. This research focuses on the use of modified pullulan for the preparation of polymeric liposomes of FTC. Modified pullulan was synthesized using cholesterol, and succinic anhydride in a controlled chemical environment. The formation of the polymer was established through analysis of spectra. Varying the drug-polymer ratio (1:1, 1:2, and 1:3), the drug-polymer composite was loaded in the vesicular system of soya phosphatidylcholine and cholesterol. Formulations were evaluated for drug entrapment, particle size, surface morphology, and in vitro and ex vivo drug release. An in vivo study of the pure drug and the best formulation on mice was conducted for 28 days following daily oral administration to evaluate the effect on liver and hematological parameters. The best formulation was further subjected to cytotoxicity study on hepatic cell lines. Spectral analysis confirmed the formation of modified pullulan. All formulations showed high drug entrapment in the nanovesicles. The in vitro and ex vivo drug release profiles depicted a controlled release of the drug. Hematological parameters were found to be under control in the animals throughout the experimentation. A comparative histopathology study on the livers and cytotoxicity study on hepatic cell lines revealed the safety of the best formulation over the pure drug. Hence it can be concluded that polymeric liposomes of FTC can be a promising mode of delivery to overcome its limitations.

Liposomes and niosomes production by a supercritical CO2 assisted process for topical applications: A comparative study

A supercritical CO2 assisted process was used to perform a comparative study between liposomes and niosomes. Process operating conditions were fixed at 100 bar and 40 °C, and the produced vesicles were characterized in terms of mean diameter, size distribution, ζ-potential, and stability over time. Mean diameters of liposomes and niosomes were similar (130 ± 37 nm for liposomes and 141 ± 36 nm for niosomes) and both systems were stable after 1 month from production. Ascorbic acid (AA) was loaded in both kinds of formulation. AA encapsulation efficiency was equal to 92 % and 99 % for liposomes and niosomes, respectively, and DPPH-activity was larger than 90 % in both vesicular systems. Drug release tests revealed that AA was released in 120 min and 240 min from liposomes and niosomes, respectively, due to a different compactness of the vesicle bilayer.

A Comprehensive Review on Niosomes in Drug Delivery and Recent Advancements

The recent emphasis on nanocarrier development for drug delivery stems from the need to target specific diseased areas while sparing healthy tissues. Effective and safe drug administration has long posed challenges in medicine. Over the past decade, the emergence of vesicles as a means to enhance drug delivery has captivated researchers in the field of drug delivery systems. Among vesicular systems, niosomes have gained attention due to their nonionic features. Unlike liposomes, niosomes offer superior stability, making them a preferred choice. Non-ionic in nature niosomes offer unique advantages in drug delivery providing a versatile platform for encapsulating various drugs to enhance bioavailability and ensure controlled release. Understanding preparation techniques enables tailored applications from oral to transdermal delivery. Characterization methods such as morphology and particles size are pivotal in ensuring the stability and effectiveness of niosomes. Applications span cancer therapy, diagnostic imaging, and vaccination adjuvants, showcasing niosomes versatility. Ongoing research reflects dynamic efforts to enhance capabilities, emphasizing their pivotal role in evolving drug delivery systems. In this comprehensive review, we aim to encapsulate fundamental aspects of niosomes, encompassing diverse preparation methods, various niosomal types, methods for characterization and the advancements witnessed in niosomal research over the past decade, drawing insights from a literature review. Keywords: Niosomes, Drug delivery, Nanocarrier, Vesicles, Nanomedicines

Antimicrobial and Anesthetic Niosomal Formulations Based on Amino Acid-Derived Surfactants.

This work proposes the development of new vesicular systems based on anesthetic compounds (lidocaine (LID) and capsaicin (CA)) and antimicrobial agents (amino acid-based surfactants from phenylalanine), with a focus on physicochemical characterization and the evaluation of antimicrobial and cytotoxic properties. Phenylalanine surfactants were characterized via high-performance liquid chromatography (HPLC) and nuclear magnetic resonance (NMR). Different niosomal systems based on capsaicin, lidocaine, cationic phenylalanine surfactants, and dipalmitoyl phosphatidylcholine (DPPC) were characterized in terms of size, polydispersion index (PI), zeta potential, and encapsulation efficiency using dynamic light scattering (DLS), transmitted light microscopy (TEM), and small-angle X-ray scattering (SAXS). Furthermore, the interaction of the pure compounds used to prepare the niosomal formulations with DPPC monolayers was determined using a Langmuir balance. The antibacterial activity of the vesicular systems and their biocompatibility were evaluated, and molecular docking studies were carried out to obtain information about the mechanism by which these compounds interact with bacteria. The stability and reduced size of the analyzed niosomal formulations demonstrate their potential in pharmaceutical applications. The nanosystems exhibit promising antimicrobial activity, marking a significant advancement in pharmaceutical delivery systems with dual therapeutic properties. The biocompatibility of some formulations underscores their viability. The proposed niosomal formulations could constitute an important advance in the pharmaceutical field, offering delivery systems for combined therapies thanks to the pharmacological properties of the individual components.

Repurposing of Nano-Engineered Piroxicam as an Approach for Cutaneous Wound Healing

Drug repurposing is a potential strategy to overcome the huge economic expenses of wound healing products. This work aims to develop a topical gel of piroxicam encapsulated into a nanospanlastics vesicular system as an effective, dermal wound dressing. Firstly, piroxicam was entrapped into nanospanlastics formulations and optimized utilizing 23 full factorial experimental designs. The scrutinized factors were Span 60: Edge activator ratio, edge activator type, and permeation enhancer type. The measured responses were vesicle size (VS), polydispersity index (PDI), and% entrapment efficiency (EE). The optimized formula was further adopted into an alginate-pectin gel matrix to maximize adherence to the skin. The rheology and in-vitro release were studied for the developed nanospanlastics gel. Cytotoxicity and wound healing potential using scratch assay were assessed on human adult dermal fibroblast cells. The optimal piroxicam nanospanlastics formula demonstrated a VS of 124.1 ± 1.3 nm, PDI of 0.21 ± 0.01, and EE% of 97.27±0.21%. About 70.0 ± 0.9% and 57.4 ± 0.1% of piroxicam were released from nanospanlastics dispersion and gel within 24 h, respectively. Nanospanlastics gel of piroxicam flowed in a non-Newtonian pseudoplastic shear thinning pattern. It was also biocompatible with the human dermal fibroblast cells and significantly promoted their migration rate which suggests an auspicious cutaneous wound healing aptitude.

Nanosphere Precision: Emulsomes Revolutionizing Cancer Targeted Therapy

Abstract: Emulsomes have gained attention because they are a novel lipoidal vesicular system that has an internal solid fat core surrounded by a phospholipid bilayer. Cancer is a complex and broad term that refers to a group of diseases characterized by the uncontrolled growth and spread of abnormal cells in the body. In the context of cancer targeting, emulsomes have shown promising potential due to their ability to improve the solubility, stability, and bioavailability of anticancer drugs, leading to enhanced therapeutic efficacy and reduced systemic toxicity. This article addresses emulsomal composition, preparation techniques, and different kinds of emulsomes loaded with drugs like fluvastatin and raloxifene hydrochloride to target cancer cells. The use of emulsomes in cancer targeting holds great promise for improving the precision, efficacy, and safety of cancer treatments. A comprehensive search of relevant scientific literature was performed. This involved searching databases such as PubMed, Scopus, Web of Science, and others to identify relevant studies, articles, and reviews related to the topic. Emulsomes loaded with specific drugs show promising results in cancer treatment. Examples include piceatannol-loaded emulsomes for colon cancer, raloxifene hydrochloride-loaded emulsomes for breast cancer, and fluvastatin-loaded emulsomes for prostate cancer. Emulsomes represent a cutting-edge approach to cancer drug delivery, offering a versatile and effective solution to address challenges associated with traditional anticancer formulations. Ongoing research holds promise for the continued development of personalized cancer therapy.

Emerging Trends in Novel Drug Delivery Systems for the Effective Treatment of Oral Cancer

Background: The consumption of tobacco and alcohol has been correlated with the development of oral cancer, impacting various areas such as the mouth, lips, tongue, cheeks, and throat. This condition is marked by irregular cell proliferation involving intricate genetic and epigenetic alterations that drive tumorigenesis. Traditional treatments face limitations, necessitating a comprehensive multidisciplinary strategy. Novel Drug Delivery Systems [NDDS] offer groundbreaking therapeutic possibilities in addressing this complex health challenge. Objective: This review emphasizes the use of NDDS in the treatment of oral cancer Methods: The review entailed a comprehensive exploration of scientific databases and pertinent publications, encompassing studies conducted up to the current date sourced from PubMed, Science Direct, and Google Scholar Key. The search terms incorporated "oral cancer," "novel drug delivery system," "chemotherapy," "nanotechnology," and "conventional therapy." The chosen studies underwent meticulous assessment for methodological robustness and the importance of their findings. Results: NDDS serve an important role in targeted medication delivery by increasing drug bioavailability and reducing adverse effects. Addressing challenges such as low drug solubility, NDDS excels in sustained release methods, guaranteeing long-term therapeutic impact. Their versatility extends to the encapsulation of several anticancer drugs, giving a potential option for oral cancer treatment that is both efficacious and well-tolerated. This novel technique has the potential to transform treatment approaches, improving the efficacy and tolerability of oral cancer drugs. Conclusion: In oral cancer treatment, a spectrum of drug delivery systems is employed, encompassing conventional methods like oral and intravenous administration alongside innovative approaches such as vesicular systems, polymeric systems, and targeted strategies. Recent breakthroughs in oral cancer therapy, including immunotherapy [checkpoint inhibitors, CAR-T cell therapy] and gene therapy [siRNA, miRNA, CRISPR-Cas9], offer exciting prospects. These advancements hold the potential for enhanced therapeutic efficacy, minimized side effects, and personalized treatment options.

Preparation and Evaluation of Fenticonazole Nitrate Loaded Topical Emulgel for the Treatment of Cutaneous Candidiasis

Fenticonazole nitrate is a broad-spectrum antifungal agent possessing fungicidal, antiparasitic, and fungistatic activities. It is effective against various fungi, including Candida species, dermatophytes, and Trichomonas, which are associated with skin and vaginal infections. Emulgel systems have gained significant attention as topical drug delivery vehicles due to their ability to incorporate a wide range of therapeutic molecules, including both hydrophobic and hydrophilic drugs. The primary objective of this study was to develop an emulgel formulation of fenticonazole nitrate for the treatment of cutaneous candidiasis (cutaneous moniliasis). Conventional emulsions often face stability issues during manufacturing and storage, which can impact drug release patterns. To overcome these challenges, the emulsion was incorporated into a gel base to enhance stability. Emulgels offer significant advantages over traditional and newer vesicular systems, such as improved therapeutic efficacy, higher drug entrapment capacity, better physiological and biological compatibility, and enhanced stability. In this study, the primary oil-in-water (o/w) emulsion was prepared using a surfactant and co-surfactant mixture (3:1 ratio) incorporated with light liquid paraffin. After characterization and optimization, the final emulsion batch was mixed with the gelling agent HPMC K4M (1:1 ratio) to obtain the emulgel formulation. The optimized emulgel exhibited optimal drug release and satisfactory results in various evaluation parameters, making it a promising topical delivery system for fenticonazole nitrate in the treatment of cutaneous candidiasis

Revolutionizing Stroke Care: Nanotechnology-Based Brain Delivery as a Novel Paradigm for Treatment and Diagnosis.

Stroke, a severe medical condition arising from abnormalities in the coagulation-fibrinolysis cycle and metabolic processes, results in brain cell impairment and injury due to blood flow obstruction within the brain. Prompt and efficient therapeutic approaches are imperative to control and preserve brain functions. Conventional stroke medications, including fibrinolytic agents, play a crucial role in facilitating reperfusion to the ischemic brain. However, their clinical efficacy is hampered by short plasma half-lives, limited brain tissue distribution attributed to the blood-brain barrier (BBB), and lack of targeted drug delivery to the ischemic region. To address these challenges, diverse nanomedicine strategies, such as vesicular systems, polymeric nanoparticles, dendrimers, exosomes, inorganic nanoparticles, and biomimetic nanoparticles, have emerged. These platforms enhance drug pharmacokinetics by facilitating targeted drug accumulation at the ischemic site. By leveraging nanocarriers, engineered drug delivery systems hold the potential to overcome challenges associated with conventional stroke medications. This comprehensive review explores the pathophysiological mechanism underlying stroke and BBB disruption in stroke. Additionally, this review investigates the utilization of nanocarriers for current therapeutic and diagnostic interventions in stroke management. By addressing these aspects, the review aims to provide insight into potential strategies for improving stroke treatment and diagnosis through a nanomedicine approach.

Current developments in Niosomes: Brand new extended release- An Introduction to Nonionic Stable Vesicular Systems

Vesicular systems are an innovative way to distribute drugs in a controlled way, improving bioavailability and achieving a longer-lasting therapeutic effect. When non-ionic surfactant vesicles self-assemble, niosomes are formed. The niosome formation is influenced by a number of variables, including the kind of non-ionic surfactant utilized, the preparation technique, the hydration temperature, etc. We have tried to include all the fundamental information about niosomes in this review article, including the different preparation techniques, types of niosomes, Advantages and disadvantages, niosome characterization, applications, and Drug delivery via niosomes. Lastly, the delivery system's limitations and prospects have also been covered.

Transferosome- A Noval Drug Delivery System

The skin's barrier function typically places restrictions on the transdermal administration of medications. One of the most contentious techniques for transdermal distribution of active ingredients is vesicular systems. After elastic vesicles such as transferosomes, ethosomes, cubosomes, phytosomes, etc. were discovered, there was a renewed interest in developing transdermal delivery systems. In order to provide active compounds transdermally, this paper describes the composition, penetration mechanisms, production processes, and characterization techniques of transferosomes. A medication must cross one or more biological membranes or barriers at different sites in order to be absorbed, distributed into organs and tissues, and removed from the body. Substance transport refers to the passage of a substance through a membrane in this manner. The medications must get through the membranous barrier in order to be absorbed by the body. In an effort to reduce the amount of medicine in the remaining tissues and concentrate the drug in the targeted tissues, several delivery systems were devised. As a result, the medication has no effect on the tissues nearby. Furthermore, medication loss does not occur. Furthermore, the localization of the drug prevents drug loss, resulting in the medication's optimum efficacy. As such, there is a lot of interest in phospholipid-based carrier systems nowadays.

Beyond Traditional Sunscreens: A Review of Liposomal-Based Systems for Photoprotection.

Sunscreen products are essential for shielding the skin from ultraviolet (UV) radiation, a leading cause of skin cancer. While existing products serve this purpose, there is a growing need to enhance their efficacy while minimizing potential systemic absorption of UV filters and associated toxicological risks. Liposomal-based formulations have emerged as a promising approach to address these challenges and develop advanced photoprotective products. These vesicular systems offer versatility in carrying both hydrophilic and lipophilic UV filters, enabling the creation of broad-spectrum sunscreens. Moreover, their composition based on phospholipids, resembling that of the stratum corneum, facilitates adherence to the skin's surface layers, thereby improving photoprotective efficacy. The research discussed in this review underscores the significant advantages of liposomes in photoprotection, including their ability to limit the systemic absorption of UV filters, enhance formulation stability, and augment photoprotective effects. However, despite these benefits, there remains a notable gap between the potential of liposomal systems and their utilization in sunscreen development. Consequently, this review emphasizes the importance of leveraging liposomes and related vesicular systems as innovative tools for crafting novel and more efficient photoprotective formulations.

Desosomes and desimicelles − a novel vesicular and micellar system for enhanced oral delivery of poorly soluble drug: Optimization of in vitro characteristics and in vivo performance

This study introduces two innovative nanocarrier systems to improve oral drug delivery. Desosomes and desimicelles combine Deep eutectic solvent (DES) with vesicular or micellar nanosystems, respectively. These novel nanosystems integrate the DES solubilization potency for administering drugs with low aqueous solubility and the vesicular and micellar systems to bypass physiological barriers and improve poor drug bioavailability. Lornoxicam (LRX) is a BCS class II anti-inflammatory with limited aqueous solubility and rapid clearance. Desosomes and desimicelles were prepared and successfully optimized. The optimization depended on particle size, zetapotential, entrapment efficiency, and solubility. The optimized desosomes (LRX-DES-V) and desimicelles (LRX-DES-M) were pictured by transmission electron microscope. Differential scanning calorimetry (DSC) and FTIR analysis indicated the successful inclusion of LRX inside each system. Invitro LRX release profiles revealed controlled release of LRX-DES-V and LRX-DES-M, with more sustained release by the later one. In-vivo study, inflammation was induced using a carrageenan rat model, and the anti-inflammatory effect of LRX-pure, marketed product, traditional niosomes, LRX-DES-V & LRX-DES-M were determined using inhibition %, serum inflammatory cytokines, and histopathology. After 4 h of induction, LRX-DES-M (68.05%) showed a significant inhibition compared to LRX-DES-V (63.57%). LRX-DES-M also showed a better reduction in COX2, PGE2, and TNF-α (1.25-fold, 1.24-fold, and 1.36-fold inhibition), respectively, compared to LRX-DES-V. We can conclude that LRX-DES-V and LRX-DES-M showed better effects than all other groups and that LRX-DES-M might be more effective than LRX-DES-V.

Comparative evaluation of pharmacokinetic parameters between a pure nisoldipine suspension and a nisoldipine-loaded bilosome suspension

Bilosomes are nanocarriers that contain bile salts in their vesicular bilayer, thereby enhancing their flexibility and durability in the gastrointestinal tract. Unlike conventional vesicular systems they provide distinct advantages such as streamlined manufacturing procedures, cost efficiency, and improved stability. The main objective of this study was to attain a comparison of the pharmacokinetic parameters of nisoldipine (NSD) after administering an ordinary NSD suspension and an NSD-loaded bilosome suspension. The study used 60 Swiss albino rats weighing 200±15 g and divided into two groups (n=30 each). A dose of 2.2 mg/kg of NSD was administered from the ordinary NSD suspension to the rats of the first group and the same dose of NSD-loaded bilosome suspension was administered to the rats of the second group. NSD levels were determined in the rat plasma by using high-performance liquid chromatography. Our results showed that the Cmax, the Tmax, and the AUC0-36 were 51.47±0.94 ng/mL, 2±0.3 h, and 323.33±21 ng×h/mL for the pure suspension, and 116.41±1.22 ng/mL, 4±0.7 h, and 916±64.09 ng×h/mL for the bilosome suspension, respectively. The maximum concentration was significantly different between the pure and the bilosomal preparation (P<0.05), while the relative bioavailability of the pure suspension was 2.9 times that of the bilosomal suspension, 36 h after a single-dose NSD administration. In conclusion, the prepared bilosomal suspension enhanced the bioavaila¬bility of NSD, and could be considered as a vital delivery system.

LATEX AGGLOMERATION AND COAGULATION IN LATICIFERS OF LIVE TARAXACUM KOK-SAGHYZ (RUBBER DANDELION) ROOTS

ABSTRACT The commercialization of Taraxacum kok-saghyz (rubber dandelion) as an alternative rubber crop requires fundamental knowledge of latex, an aqueous suspension of rubber particles, and rubber yield and quality. Rubber particles are formed in the root laticifers from Golgi bodies via the vesicular trafficking system in the cytosol and are then translocated into the vacuoles for storage. However, when freshly harvested roots are processed to extract the latex, much of the latex has already coagulated into solid rubber, reducing the commercial viability of latex extraction from this species. The process of in vivo loss of the latex fraction was investigated histologically, by transmission electron microscopy, in roots of plants grown in soil or hydroponically. In both root types, some rubber particles agglomerated in the cytosol as a precursor to coagulation. Other rubber particles agglomerated and then coagulated after rubber particles were translocated into vacuoles, and also after the cell internal cytoplasmic structure degraded. Uniquely large rubber particles were formed in the vacuoles of hydroponically grown plants by particle coalescence, but were not found in soil-grown roots. Eventually, some root laticifers of both root types filled with solid rubber. The instability of the aqueous latex phase postontogeny through rubber particle agglomeration, coalescence, and coagulation suggests that commercial processes likely would involve root drying to convert residual latex into solid rubber followed by aqueous- or solvent-based extraction.