Nano Formulation Research Articles

Anticancer Analysis of CD44 Targeted Cyclosporine Loaded Thiolated Chitosan Nanoformulations for Sustained Release in Triple-Negative Breast Cancer.

Cyclosporine (CsA), a potent immunosuppressive chemotherapeutic medication, treats numerous cancers, particularly malignant carcinoma, acute leukemia, and triple-negative breast cancer (TNBC). A specified polymeric nanoformulation (NF) based drug delivery technique with ligand functionalization at the surface was developed to improve its delivery at the intended area and boost the efficacy for prolonged time. The in silico verified the HA binding to the CD44 receptor at binding sites A and B in triple-negative breast cancer cells. The NF of encapsulated Cyclosporine in thiolated chitosan (TC) with the outermost coating of hyaluronic acid (HA) was formulated and characterized. So, the zeta analysis revealed a particle size of 192 nm and PDI of 0.433, zeta potential of 38.9mV. FTIR and Raman investigations also support the existence of hydrophobic groups, porous surfaces, and non-clumping characteristics. While XRD verified its crystallographic nature while SEM and TEM analysis revealed the spherical nanoparticles with sleek exteriors. DSC demonstrated the stability of NF at high temperatures. The NF showed 85% drug encapsulation followed Higuchi release model for therapeutic moiety at acidic pH for a maximum of 72 hours. When compared to raw Cyclosporine, the in vitro tumor cell inhibition of ThC-HA encapsulated with Cyclosporine was tested using an MTT dye on normal breast epithelial cells compared to triple-negative breast cancer cells. This novel formulation improved the long-term viability, effectiveness, and active targeting as an effective and potent therapeutic moiety against cancer.

Considering the Conception of Nanotechnology Integrated on Herbal Formulation for the Management of Cancer

Abstract: Metastases result from a complicated process in which malignant cells detach from the initial cancerous cells and disseminate to other locations. Few therapy options are available that aim to prevent or counteract metastatic disorders. Identifying novel molecular targets and medications, developing techniques to distribute preexisting chemicals, and combining resources to supervise individualized treatment are all part of this process. Because of its improved sensitivity, accuracy, and multiplexed measurement capacity, nanotechnology has been investigated to recognize extracellular cancer biomarkers, cancer cells, and bioimaging. Nanotechnology is a vast and rapidly expanding field with enormous potential in cancer treatment. Nanoparticles can treat resistant cancers with minimal harm to healthy tissues and organs by targeting cancer stem cells. Nanoparticles can also trigger immune cells, which can help to destroy malignancies. The potential of herbal-based nano formulation as a specialized and high-efficacy therapeutic method opens the path for future research into the screening and use of herbal nanoparticles for cancer treatment. The possible impacts of nanoparticles in the therapy of metastatic cancer, specifically on cell stability, proliferation suppression, eventual interaction with adhesion molecules, and antiangiogenic activity, are discussed in this paper.

A Study on the Stoichiometry of Casein/Chitosan Gel Complexes as a Delivery System for Quercetin

As a well-known plant flavanol, quercetin possesses a diverse range of biological properties. These include its ability to act as an antioxidant, reduce inflammation, and exhibit anticancer effects. Consequently, it finds extensive application in numerous models related to wound healing. However, the poor physicochemical characteristics of the molecule (which include low solubility, stability, and permeability) eventually reduce its bioavailability at the targeted sites. A variety of nano formulations with great therapeutic potential have been created in order to get around these obstacles on the way to successful therapy. The current investigation aims to examine the properties of nano- and micro-sized casein/chitosan gel polyelectrolyte complexes (PECs) with respect to their potential for quercetin loading and release. Four different types of hydrogel particles at pH 6 and different casein/chitosan charge ratios were synthesized; namely, 1:1, 2:1, 4:1, and 6:1 in excesses of casein. The attractive electrostatic interactions between the oppositely charged polyelectrolytes were proved by FT-IR spectroscopy. The process yield increased from 37.5% to 72.5% in excesses of casein. The gel particle’s size varied between 377 nm and 5.72 µm depending on the casein/chitosan stoichiometry. The morphology of the obtained gel polyelectrolyte complexes was found to be spherical, based on scanning electron microscopy and atomic force microscopy analysis. The quercetin loading efficiency was above 95% for all investigated hydrogel complexes. Investigation of the physical state of the loaded polyphenol by the differential scanning calorimetry and X-ray powdered diffraction technique suggested the occurrence of partial recrystallization phenomena. The quercetin release test was performed in phosphate buffer (pH 5.5) at 32 °C and permanent stirring at 50 rpm. A zero-order model was used to describe in the best way the release kinetics. The reported casein/chitosan complexes loaded with quercetin may find application in wound healing as a concomitant treatment.

Phytochemicals and Therapeutic Potential of Pomegranate

A significant source of polyphenolic chemicals is the pomegranate (Punica granatum). Due to the several pharmacological functions attributed to its phytochemicals, it has been gaining importance. An extensive list of the phytoconstituents present in pomegranate fruits, peel, blossoms, and seeds as well as their pharmacological actions were the goals of this in-depth analysis. The flavonoids and tannins (gallotannin and ellagitannin), which are the active phytochemicals in pomegranate extract, are what give it its anti-inflammatory, antioxidant, anti-angiogenic, and anti-aging qualities. Pomegranate bioactive components are used industrially to create foods with additional value. Wide-ranging applications for its reducing properties in the creation of nano formulations. Its phytoconstituents may play a safer role in managing environmental contamination than the use of pesticides or other chemicals. The numerous human clinical investigations assessing its pharmacological importance have received special attention.

Nano-phototherapy: Favorable prospects for cancer treatment.

Nanotechnology-based phototherapies have drawn interest in the fight against cancer because of its noninvasiveness, high flexibility, and precision in terms of cancer targeting and drug delivery based on its surface properties and size. Phototherapy has made remarkable development in recent decades. Approaches to phototherapy, which utilize nanomaterials or nanotechnology have emerged to contribute to advances around nanotechnologies in medicine, particularly for cancers. A brief overviews of the development of photodynamic therapy as well as its mechanism in cancer treatment is provided. We emphasize the design of novel nanoparticles utilized in photodynamic therapy while summarizing the representative progress during the recent years. Finally, to forecast important future research in this area, we examine the viability and promise of photodynamic therapy systems based on nanoparticles in clinical anticancer treatment applications and briefly make mention of the elimination of all reactive metabolites pertaining to nano formulations inside living organisms providing insight into clinical mechanistic processes. Future developments and therapeutic prospects for photodynamic treatments are anticipated. Our viewpoints might encourage scientists to create more potent phototherapy-based cancer therapeutic modalities. This article is categorized under: Therapeutic Approaches and Drug Discovery > Nanomedicine for Oncologic Disease.

Dasatinib and Hesperidin Loaded Nano Formulation and Preclinical Evaluation for Anticancer Activity

In this study, we aimed to develop Dasatinib/hesperidin-loaded-SLNs for chronic myeloid leukemia (CML). Utilizing a high-shear homogenizer for the synthesis, “central composite design (CCD)” was used to enhance the dasatinib/hesperidin loaded-SLNs. The optimized SLNs had PDI, particle size, and average entrapment efficiency of 0.12%, 162.3 nm, and 93%, respectively. Therefore, by enhancing the total amount of Compritol as well as sonication time the polydispersity was increased. Poloxamer 188 content had a significant influence in decreasing the polydispersity index and the entrapment efficiency (EE) of the SLN was found to be 93%. Through TEM, SEM, FTIR, DSC, and HPLC analysis, SLNs were characterized, and their anticancer efficiency was assessed in both in-vitro and in-vitro cell viability tests (MTT). SLNs containing dasatinib and hesperidin have rounded and spherical shape having a diameter of 200 nm. DSC and FTIR tests showed compatibility between the drugs and excipients. The drug release from optimized SLN formulation was under observation for 48 hours. It was found that the medication released its drug components over a protracted period of time, with 30% of the drug being released in the first four hours and the remainder 76% in the next 48 hours. According to the IC50 values determined by an independent study, dasatinib, hesperidin, and SLN were 33.97, 5158, and 4.03 μg/mL, respectively. A comparison of SLN and free drugs revealed that SLN was more effective at cytotoxicity. In this study, dasatinib and hesperidin-loaded SLNs for chronic myeloid leukemia (CML) against HL60 human leukemia cell lines were prepared and evaluated using a novel formulation approach free of toxic excipients.

Design and synthesize of folate decorated Fe3O4@Au-DEX-CP nano formulation for targeted drug delivery in colorectal cancer therapy: In vitro and in vivo studies

Design and synthesize of folate decorated Fe3O4@Au-DEX-CP nano formulation for targeted drug delivery in colorectal cancer therapy: In vitro and in vivo studies

Efficacy of Non-Conventional Chemical Inducers against Fusarium oxysporum Inciting Wilt in Chilli

Chilli wilt incited by Fusarium oxysporum is the most devastating disease, causing substantial yield losses throughout chilli growing areas of the world. Fusarium oxysporum is a soil-borne fungus which survives for several years in soil. The disease is favoured by high temperature and high moisture, this condition plays significant role in development of wilt symptoms. The disease management using chemicals is economically not feasible and is also unsafe for the environment. Due to growing public awareness to environment and human health, need of the hour is to find alternate approaches for disease management. Therefore, to investigate induction of systemic resistance against Fusarium oxysporum in chilli. Different non-conventional chemical inducers like salicylic acid (SA), jasmonic acid (JA), Indole acetic acid (IAA), Indole butyric acid (IBA), chitosan, salicylic acid nano formulation and chitosan nano formulation were used in an experiment conducted in Department of plant pathology, Chaudhary Charan Singh Haryana Agricultural University, Hisar, Haryana. These non-conventional chemicals with four concentrations 25, 50, 75 and 100 µg/ml were evaluated for their antifungal activity against Fusarium oxysporum under in vitro condition using poison food technique with four replications. It was found that the highest mycelial growth inhibition was observed in salicylic acid nano formulation (79.73%) at 100 µg/ml concentration followed by Jasmonic acid (77.12%) at 100 µg/ml concentration and the lowest growth inhibition was recorded in Indole acetic acid (27.15%) at 100 µg/ml concentration. The same trend was observed when chilli varieties Pusa Jwala (susceptible) and Pusa Sadabahar (moderately resistant) were tested with the two best and the least effective non-conventional chemical inducer obtained in vitro for measuring the disease severity in screen house. This insight clarifies the scope of using non-conventional chemical inducers as an effective disease management strategy against Fusarium wilt of chilli.

Development of eco-friendly natural formulation for management of resistant tick infesting animals and humans

Almost all livestock species are suffering from tick infestations. Ticks are voracious blood suckers, causing significant blood loss in livestock resulting low productivity in terms of weight gain and milk yield, increased mortality and low-quality hides. Ticks also serve as the major vector of economically important diseases like babesiosis, theileriosis and anaplasmosis. The use of synthetic acaricides of different classes is the backbone of tick management programme. But indiscriminate application of these chemicals has led to the development of resistance against commonly used synthetic acaricides. It is become a challenging task to manage tick infestations using existing resources. The present study was undertaken to develop green nano formulation for mitigation of the resistant problem. The characterized green nano-formulation may be a suitable alternative to minimize the excessive use of chemical acaricides. The use of synthetic acaricides of different classes is the backbone of tick management programme. But the indiscriminate application of these chemicals has led to the development of resistance against commonly used synthetic acaricides.

Nanostructured lipid carriers of ivabradine hydrochloride: Optimization, characterization and in-vivo estimation for management of stable angina

Stable angina (angina pectoris) is a type of chest pain that happens when the heart muscle needs more oxygen than usual but it's not getting it at that moment because of heart disease. The drawback of the marketed formulation is required repeated administration of the drug due to low bioavailability. A recently licenced medication called ivabradine hydrochloride (IVB) is used to treat stable angina and signs of heart failure. Technical problems in the approved IBH tablets include a two-hour half-life, erratic systemic absorption, and a high rate of first-pass metabolism (>50%). We therefore created a distinctive and cutting-edge formulation of IVB using a nano formulation approach like nanostructured lipid carriers (NLCs). The response surface method with a three-level Box–Behnken design was used for the creation and improvement of IVB. The optimized formulation was proceeded for physicochemical characterizations like particle size, zeta potential, morphology (TEM and SEM), entrapment efficiency, in-vitro release, stability studies, compatibility study (DSC, FTIR and XRD), hemocompatibility study, ex-vivo permeability, and in-vivo angina study. As results, optimized formulation was found to be 114.45 ± 5.14 nm particle size with 83.45 ± 3.23% entrapment efficiency and biphasic release. The formulation showed spherical and compatible with excipients, no interaction was observed and hemocompatible. The IBH-NLCss showed more permeability (1.85 folds) as compared to the marketed dosage form. The in-vivo pharmacological activity was established in terms of decrease in severity and duration of ST-segment depression in vasopressin-induced angina model in experimental rats.

Formulation and Evaluation of Aspirin Nanosuspension Using Probe Sonication Method

Aspirin inhibit the activity of the enzyme now called cyclooxygenase (COX) which leads to the formation of prostaglandins (PGs) that cause inflammation, swelling, pain and fever. Aspirin having various function like anti-inflammatory, analgesic, antipyretic etc. Aspirin loaded nanosuspension was prepared to enhance the bioavailability of the drug. Nanosuspension is defined as a finely dispersed solid particle dissolved in aqueous and organic medium for oral, tropical, parenteral or pulmonary administration. The size ranges about 200nm to 600nm.Aspirin loaded nanosuspension was prepared by probe sonication method. The probe sonication method is used to reduce the particle size and to increase the solubility of the drug. Total 5 Nano formulations were prepared in which NS1 shows 100% of drug content. Invitro Drug release was performed using Franz diffusion cell in which NS5 formulation shows 94.7% drug release in a time period of two hours and 30 minutes. Entrapment efficiency was performed using Ultracentrifugation method kept for 40 minutes at 17,000 rpm speed. Among all NS5 shows 71.9% of entrapment efficiency.

A story of Shigella vaccine development in ICMR-NICED involving multidimensional approaches

Enteric bacterial infection causes diarrhea throughout the world, especially in developing countries. Shigella is solely answerable toalmost 1.1 million deaths annually in the pediatric population. Vaccine development against diarrheal diseases is always an encouragedconcern. Our laboratory, dedicated to find a possible therapy against shigellosis, is working on a path of various potential methodologiesand immunogens. Over the years, we have concentrated and reported different immunogens with their advantages and drawbacks,ultimately leading us to find the best possible vaccine candidate against bloody diarrhea.The venture started with live attenuated vaccines that protect against multiple serotypes and subtypes of pathogens and found limitedhost-serotype specific immune responses. It was observed that introducing a lipopolysaccharide biosynthesis gene pPR 1347 in Shigelladysenteriae type 1, transformed it into an avirulent organism for candidate vaccine.A mutant strain of Shigella flexneri 2a lacking the RNA-binding protein Hfq was made, leading to increased expression of the type IIIsecretion system via loss of regulation, resulting in attenuation of cell viability through repression of stress response sigma factors. Suchincreased antigen production and simultaneous attenuation were expected to elicit protective immunity against homologous and alimited number of heterologous serotypes subtypes.Although we formulated the live attenuated vaccine through the introduction of a lipopolysaccharide gene and a mutant lackingRNA binding protein Hfq, but due to lack of heterologous protective efficacy, these were not an ideal vaccine candidate to be madeavailable in the market although they showed a significant amount of immunogenicity. Moreover, live attenuated strains always havea possibility to revert back to its virulent form.Subsequently, monovalent and hexavalent heat-killed immunogens with single and six Shigella serotypes have shown significantprotective efficacy in mice, and rabbit models. Recently we have shown the homologous as well some extent of heterologus protectiveefficacy of heat killed multi-serotype Shigella (HKMS) immunogens in a guinea pig colitis model.A novel formulation for improved immunogen delivery system comprises substantially effective amounts of alginate chitosannanoparticles with OmpA protein of Shigella species. Alginate chitosan nano formulations of OmpA consists essentially of OmpAprotein as conserved active molecule, but efficacy study reveals partial protection efficacy against present circulating Shigella. Furtherimproving the delivery system, we have also formulated a subunit-based vaccine by nanoformulation of ipaC protein of Shigella. Themain drawback of OmpA and ipaC subunit based vaccines are they cannot provide a broad spectrum protection against 50 subtypesand serotypes of Shigella, although they act as a conserved protein in Enterobacteriaceae family, indicating single epitope cannot bethe sole factor associated with the operational protective efficacy.Eventually, our research moved a step ahead and found next-generation outer membrane vesicles (OMVs) based antigens from Shigella.Disruption of tolA, one of the genes of the Tol–Pal system of Shigella membrane, has increased the OMVs release rate by approximately80% higher. Recently we have reported only four serotype-subtype cross-protection among 50 subtypes of circulating Shigella in micemodels. Outer membrane vesicles based immunogen could be a potential cost-effective non-living, next-generation candidate vaccineagainst shigellosis for humans.

Nanomaterials and Diverse Agricultural Applications: A Comprehensive Review

Climate change, the population explosion and the growing demand for good food and health require better, more reliable and more efficient. The different shape, size, composition and ability to interact with organic compounds make nanomaterials and technology widely used. Nano formulations and their applications in agriculture in the form of agrochemicals for crop protection, toxicity identification by nanobiosensors, genetic manipulation of plants treated by nanodevices, and rapid and efficient diseases of plants. The delivery of genetic material and proteins via nano-arrays has been proven in crop engineering, drug delivery and environmental monitoring. Nanotechnology also benefits the food industry by improving all stages of food production from food processing to production, processing, packaging, safety, extending shelf life, testing for disease and creating smart foods. Therefore, technology can meet the needs of most consumers, including the improvement of food products and their sensations, and can improve product quality, texture soft and nutritious food without affecting its natural properties.

A Comprehensive Review on Nanophytomedicines and their Applications

Among natural sources we mainly consider the plant-based phytochemicals. Phytochemicals or the secondary metabolites are the extract obtained from the herbal plants which may serve as a great venture for their utilization as nanomedicine. Drugs or compounds converted to nano range shows unique characteristics which lengthen circulation, ameliorate localization, improve drug efficiency, etc. Nanomedicine is the type of formulation which uses the nanotechnology to deliver the drug in the form of nanoparticles incorporated within the nanocarriers. Nanocarriers intensify solubility and stability of phytochemicals, prolong their half-life in blood and achieve sitetargeting delivery. The development of phyto-based nano formulations has been explored to have potential applications in managing life-threatening diseases. The present review highlights the compilation on the potential of phyto nanotherapeutics over the conventional treatments against various serious leading disorders. Dhaka Univ. J. Pharm. Sci. 22(1): 115-124, 2023 (June)

RETRACTED ARTICLE: Evaluation of the anticancer potential of CD44 targeted vincristine nanoformulation in prostate cancer xenograft model: a multi-dynamic approach for advanced pharmacokinetic evaluation

The in vivo anticancer potential of vincristine (VC) loaded, thiolated chitosan-based nanoformulation (NFs) with an outer hyaluronic acid (VC-loaded in TCs-HA) coating was studied in prostate cancer (PC) xenograft in the immunosuppressed rat model induced by PC3 cell lines. Our previous study has already reported the in vitro efficacy of the said NFs. The ADMET Predictor (TM) Cloud version 10.4.0.5, 64-bit, was used to simulate VC's physicochemical and pharmacokinetic parameters. The percentage of encapsulation efficiency of VC by direct and indirect methods was 81.5 and 90%, respectively. Plasma samples from healthy rats showed improved pharmacokinetic and bioavailability profiles of NFs compared to VC injection via HPLC. The haemolytic analysis of NFs showed two times lesser toxicity to red blood cells. Xenograft rats showed maximum tumour volume up to 235 ± 0.02 mm3 with increased body weight, and it was reduced by 56 ± 0.01 to 107.3 ± 0.03 mm3 during the whole treatment by NFs compared to pure VC. The histopathology of the NFs group showed less malignancy with angiogenesis and significantly less metastasis to the liver and kidney. ELISA showed high expression of apoptotic biomarkers, including Bax, cleaved Caspase 3, and cleaved PARP, while the expression of BCL2, Caspase 3, COX-II, NFκB, and TNF-α was reduced. Immunohistochemical analysis also revealed that post-NF administration, cytoplasmic expressions of TNF-α and COX-II were reduced, as were nuclear expressions of NFκB. Thus, the prepared chemotherapeutic NFs were a comparatively potent oncolytic agent, safe with lesser off-target toxicity, and had an improved pharmacokinetic and bioavailability profile.

Quality-by-design driven analytical method (AQbD) development and validation of HPLC–UV technique to quantify rivastigmine hydrogen tartrate in lipidic nanocarriers: Forced degradation, and assessment of drug content and in vitro release studies

The main purpose of current investigation was to design and further validate a technique for the quantitative determination of rivastigmine hydrogen tartrate (RHT), a cholinesterase inhibitor in the nano formulations. With the employment of a reverse phase C18 column and a very simple mobile phase, an isocratic HPLC–UV analysis technique was developed, optimized, and validated following ICH Q2 (R1) requirements along with the inculcation ofAnalytical Quality-by-Design (AQbD) methodology. A two-level full factorial screening design was applied to filter out the variables influencing responses, followed by the application of central composite design (CCD) to further optimize the method using Design-Expert® software. Analyses were performed at room temperature with 0.9 mL. min−1 flow rate and detection wavelength of 215 nm. The optimized HPLC technique exhibited superior linearity, selectivity, and precision. The inherent stability of RHT was evaluated using the optimized method byconductingforced degradation studies. The RHT peak was clear and unaffected by matrix interference in the specimens from the forced degradation studies, drug content analysis, and in vitro release study. The assay had a limit of detection (LOD) of 14.32 ng. mL−1 and a limit of quantitation (LOQ) of 43.40 ng. mL−1. With acceptable intra- and interday precision, the methodologywas confirmedto berobust. The devised stability-indicating HPLC technique for analyzing RHT content, its stability in the nano formulations, and drug release in vitro proved to be selective, accurate, sensitive, and consistent.

Effect of CeO2/spherical silica and halloysite nanotubes engineered for targeted drug delivery system to treat breast cancer cells

Cerium oxide nanoparticles (CeO2 NPs) and flavonoid curcumin that has been widely studied for treating diseases involving high reactive oxygen species (ROS). In nanotherapeutics, the particle size, shape, metal oxide dispersity and surface properties of nanocarriers are vital for drug delivery and therapeutic efficiency. Here, cisplatin release behavior on cerium impregnated two different shaped nanocarriers, CeO2/monodispersed spherical silica (Sil) and CeO2/halloysite (Hal) nanotube was studied for potential anti-cancer therapies. For comparison, CeO2 impregnated mesoporous silica MCM-41, SBA-16, Hydroxyapatite and clay were prepared. Subsequently, the nanocomposites were coated with curcumin (25% wt/wt), and cisplatin (Cp) functionalization (5% wt/wt). 5wt%CeO2/Hal/Cp and 5wt%CeO2/Sil/Cp samples were pegylated using lyophilization technique. Physico-chemical analyses revealed the nanosized distribution of CeO2 and functionalization of cisplatin and curcumin. Cp release was studied using automated Franz cell and dialysis membrane techniques. The different structured nanocarriers delivering mechanism was studied by determining the drug kinetic release using four different kinetic models (first order, second order, Higuchi and Korsmeyer-Peppas). In vitro cytotoxicity assay of nano formulations along with free cisplatin and curcumin (Cur) were tested against the breast cancer cell line (MCF-7) for multiple timepoints by MTT assay. The results reveled the efficacy of 5wt%CeO2/Sil/Cp/Cur nanoparticles in delivering cisplatin. On the other hand, 5wt%CeO2/Hal/Cur nanoparticles enhanced the uptake of curcumin in comparison to free curcumin. Overall, pegylated CeO2/Silica nano formulation demonstrated an effective carrier to cisplatin for potential treatment of breast cancer.

Review Development of Essential Oil Nano Preparation Formulations to Pharmacological Activity

Essential oils are liquids from the extraction process of plants or parts of aromatic plants which generally contain volatile terpenoids. This oil is characterized by distinctive odor from each plant that causes by differences in its constituent compounds. Essential oils have many pharmacological activities such as antioxidant, antibacterial etc. The development of many nano formulations has been developed, including essential oils. Nanoemulsion, nanogel, and nanoemulgel are forms of nano formulations that are applied in the manufacture of pharmaceutical preparations containing essential oils. Therefore, the purpose of this review is to present the results of the latest research on essential oil formulations using nanotechnology that have been widely developed and their effect on pharmacological activity. The articles used in this review were published from 2013-2023 which are indexed by Scopus. The formulation of essential oil preparations in nano form enhances the pharmacological effects of essential oils including increasing the effects of antioxidants, antibacterial, antifungal, antiproliferative, antiviral and reducing toxicity which can be useful as a reference for nano preparation formulations for essential oils.

Analysing the neuroprotective abilities of Apocynin (APO) & Chlorogenic Acid (CGA) in synergism to treat Alzheimer’s disease (AD)

AbstractBackgroundNeurological illnesses accounted for the greatest percentage (6.2%) of Total DALY index among all diseases, according to the World Health Organization (WHO). Alzheimer’s disease (AD) is the second most common neurological illness in the world, after Cerebrovascular disease (12 percent), with epilepsy and migraine accounting for 8% apiece. The cognitive function of people with AD deteriorates over time. It is an irreversible, dynamically changing condition that will afflict approximately 65.7 million people worldwide by 2030. For the treatment of AD, the Food and Drug Administration (FDA) has approved a number of commercial formulations (e.g., donepezil, rivastigmine, galantamine, memantine, and aducanumab). However, they have serious adverse effects and only provide symptomatic relief in people who have the illness. As a result, natural compounds are being investigated in recent years for the treatments of neurodegenerative diseases (NDDs). Picrorhiza kurroa, isolate Apocynin (APO) is a potent inhibitor of NADPH oxidase (NOX) and Chlorogenic Acid (CGA), a product of green coffee beans, has been shown to reduce ROS and NO levels in the brain, which is considered major trigger in AD.MethodIt was possible to execute successful in‐silico validation utilising computational biology, as well as the fabrication of APO‐CGA loaded polymeric nanoparticles using the ionic gelation process. The optimized nano‐formulation (APO – CGA NPs) was characterised by using various techniques to ensure its particle size and physicochemical behaviour along with release kinetics analysis.ResultThe attained results suggested that designed nano formulation will provide enhanced synergistic therapeutic efficacy to treat AD.ConclusionThe formulation and study of optimal APO‐CGA NPs for effective transport to the target site, their function in synergism, and their anti‐oxidative capabilities to evaluate the neuroprotective efficacy were the emphasis of this research work.

Advances in lipid-based carriers for cancer therapeutics: Liposomes, exosomes and hybrid exosomes

Cancer has recently surpassed heart disease as the leading cause of deaths worldwide for the age group 45–65 and has been the primary focus for biomedical researchers. Presently, the drugs involved in the first-line cancer therapy are raising concerns due to high toxicity and lack of selectivity to cancer cells. There has been a significant increase in research with innovative nano formulations to entrap the therapeutic payload to enhance efficacy and eliminate or minimize toxic effects. Lipid-based carriers stand out due to their unique structural properties and biocompatible nature. The two main leaders of lipid-based drug carriers: long known liposomes and comparatively new exosomes have been well-researched. The similarity between the two lipid-based carriers is the vesicular structure with the core's capability to carry the payload. While liposomes utilize chemically derived and altered phospholipid components, the exosomes are naturally occurring vesicles with inherent lipids, proteins, and nucleic acids. More recently, researchers have focused on developing hybrid exosomes by fusing liposomes and exosomes. Combining these two types of vesicles may offer some advantages such as high drug loading, targeted cellular uptake, biocompatibility, controlled release, stability in harsh conditions and low immunogenicity.