Beta-carotene (BC), a red-colored pigment found in plants and animals, is one of the most extensively investigated carotenoids due to its provitamin-A, antioxidant, and anticancer properties. The ...anticancer activity of BC through oral administration is severely affected due to its low bioavailability and oxidative degradation. The present study aimed to formulate and characterize solid lipid nanoparticles (SLNs) of BC for enhanced bioavailability and therapeutic efficacy. Beta-carotene-loaded solid lipid nanoparticles (BC-SLNs) were prepared employing different combinations of glyceryl monostearate and gelucire. The characterization studies were performed for particle size, morphology, release behavior, and stability. BC-SLNs were also studied for
in vitro
cytotoxicity in human breast cancer cell lines (MCF-7) and pharmacokinetic studies in Wistar rats. The cytotoxicity studies confirmed that encapsulation of BC within the lipid bilayers of nanoparticles did not affect its anticancer efficacy. An improved anticancer activity was observed in BC-SLNs as compared to the free BC. BC-SLNs enhanced the bioavailability of BC on oral administration by sustaining its release from the lipid core and prolongation of circulation time in the body. Similarly, area under the curve (AUC
total
) enhanced 1.92-times more when BC was incorporated into SLNs as compared to free BC. In conclusion, solid lipid nanoparticles could be an effective and promising strategy to improve the biopharmaceutical properties of carotenoids for anticancer effects.
β-Carotene is a red–orange pigment, a known source of vitamin A and has exceptional antioxidant and free radical scavenging potential. However, uses of β-carotene in food industry are inadequate ...mostly because of their poor water solubility and low stability. Using the complex coacervation technique, the work is meant to fabricate the microcapsules of β-carotene, to examine the physicochemical properties of microcapsules and finally to evaluate the extent of stability improvement. The configuration of electrostatic complexes between whey protein isolate (WPI) and gum acacia (Acacia arabica, GA) was optimized as a function of pH, ionic strength, WPI/GA ratio, core material load and size of final micromolecules. The optimum process conditions were balanced by the ratio of wall materials WPI/GA 2.0/1.0 % and pH value 4.2. Morphological observations showed that microcapsules presented spherical shape, and smooth and continuous surface. The effective amount of encapsulated core was greater than 70 % for all formulations evaluated. In vitro release data indicated an initial burst release followed by sustained release behavior. The microstructure and viscoelastic properties of WPI and GA complex were studied using dynamic rheometer. The encapsulation method and the wall materials used in this work gave effective protection during storage and eventually resulted sustained release of bioactive while used in food matrix, at suitable conditions.
In the last couple of decades antioxidant agents have entered the health market as an easy and attractive means of managing diseases. These agents are of enormous interest for an increasingly ...health-concerned society, and may be particularly relevant for prophylaxis of a number of diseases i.e. arthritis, cancer, metabolic and cardiovascular diseases, osteoporosis, cataracts, brain disorders, etc. Antioxidants are also favorable to vascular healthiness and symbolize useful compounds because they are able to diminish overall cardiovascular risk by acting analogous to first line therapy or as adjuvants in case of failure or in situations where first line therapy cannot be used. Furthermore, well-designed trials are indeed needed to improve the therapeutic efficacy and health benefits of antioxidants. Numerous in vivo proof-of-concepts studies are offered to underline the feasibility of nanostructure system in order to optimizing the delivery of cardiovascular drugs. The present review highlights the recent approaches for management of cardiovascular disease using different vesicular and particulate carriers, including liposomes, nanoparticles, and nanoemulsions, with a primary emphasis on those which are expected to enhance the antioxidants level.
Out of many complications two major problems facing in formulation industry are poor solubility and short half-life of drugs which results into poor bioavailability after oral administration. Solid ...dosage forms are coated for a number of reasons, the most important of which is controlling the release profiles and bioavailability of the active ingredient. Thus the development of a significant dissolution procedure for drug products with limited water solubility has been a challenge to the pharmaceutical industry. Aceclofenac (Biopharmaceutical classification Class II drug) is a novel non-steroidal anti-inflammatory drugs (NSAIDs) having anti-inflammatory and analgesic properties, and is widely used in the treatment of rheumatoid arthritis, osteoarthritis, and ankylosing spondylitis. The investigation revealed that there is no official dissolution medium available in the literature. The objective of present study is to formulate film coated tablet of Aceclofenac and Chlorzoxazone having short half-life by coating with hydroxyl propyl methyl cellulose (E5 LV). Then the formulated tablets were evaluated for its physicochemical properties and in vitro release studies. The incorporation of drugs into polymer matrices is considered a valid tool in order to optimize insufficient features of the drug molecule, like solubility, stability or toxic effects. In the present work, the incorporation of aceclofenac was performed in inert HPMC and there was no chemical interaction between the drug and polymers as concluded from the FTIR studies. In the present study, parameters such as solubility, medium pH, surfactant type, dissolution behavior of formulations, stability, and discriminatory effect of dissolution testing in different dissolution mediums were studied for the selection of a proper dissolution medium. The drug showed an enhanced release rate in the dissolution media containing pH 6.8 phosphate buffer, 900 ml with 0.5 % sodium lauryl sulphate at 75 rpm for 60 min and thus was chosen as the discriminating dissolution method for film coated aceclofenac formulation. It was found that greater than 80 % of the label amount is released over 60 min.
Anthocyanin has been proven to impart several health benefits and biological functions. Though, various analytical methods have been reported for single/multi-component analysis of anthocyanins, ...found to be tedious, time consuming and difficult to reproduce. Analytical studies on specific anthocyanins for estimation using an approach of Analytical Quality by Design are scarce. USP method is only reliable for cyanidin-3-O-glucoside (CY-3-O-Glu) estimation, but exploring many disadvantage of having high buffer concentration in mobile phase system and gradient elution, hence column blockage. So there is need to develop a novel HPLC method to overcome this problem with the use organic solvents with lesser volume of buffer in isocratic mode of elution. The aim is to develop a robust and precise method for estimation of CY-3-O-Glu in biopolymer based microcapsules and tablets. The optimized method consisted of mobile phase containing solvent A and B, flow rate 0.8 mL/min with 20 min of analysis time. The method was further validated in accordance with current ICH guidelines Q2 (R
1
) and found to be highly selective for component in the presence of degradation products confirmed by Mass spectra. Therefore, the proposed method was found to be suitable for routine analysis of CY-3-O-Glu in food and pharmaceutical based formulations.
•Concurrent administration of antioxidants in chemotherapy reduces efficacy of treatment.•Administration of antioxidants should be in the form of a maintenance dose.•FDA guidelines on intake of ...antioxidants should be followed.
Several randomized clinical trials have divulged that administration of antioxidants during chemotherapy decreases the effectiveness of treatment. Hence, the characteristic feature of this article is extensive assessment of putative benefits and potential risks of natural and synthetic antioxidant supplementation, administered with chemotherapy, based upon the available preclinical and clinical data. After analyzing mixed results, it was concluded that current FDA guidelines should be followed before supplementing antioxidants during cytotoxic treatment. Nevertheless, contradictory experimental animal models opposing human clinical trials discourage the concurrent administration of antioxidants ostensibly owing to the possibility of tumor protection and reduced survival.
•Surface engineered solid lipid nanoparticles (SLNs) encapsulated with Doxorubicin (DOX) has been successfully synthesized.•Cytotoxicity of DOX incorporated SLN was higher than plain drug solutions ...on A549 cells.•The higher efficacy of DOX incorporated SLN related to marked uptake and accumulation in the cells.
The present investigation reports the preparation, optimization, and characterization of surface engineered solid lipid nanoparticles (SLNs) encapsulated with doxorubicin (DOX). Salient features such as biocompatibility, controlled release, target competency, potential of penetration, improved physical stability, low cost and ease of scaling-up make SLNs viable alternative to liposomes for effective drug delivery. Galactosylation of SLNs instructs some gratifying characteristic, which leads to the evolution of promising delivery vehicles. The impendence of lectin receptors on different cell surfaces makes the galactosylated carriers admirable for targeted delivery of drugs to ameliorate their therapeutic index. Active participation of some lectin receptors in immune responses to antigen overlaid the application of galactosylated carriers in delivery of antigen and immunotherapy for treatment of maladies like cancer. These advantages revealed the promising potential of galactosylated carriers in each perspective of drug delivery. The developed DOX loaded galactosylated SLNs formulation was found to have particle size 239±2.40nm, PDI 0.307±0.004, entrapment efficiency 72.3±0.9%. Higher cellular uptake, cytotoxicity, and nuclear localization of galactosylated SLNs against A549 cells revealed higher efficiency of the formulation. In a nutshell, the galactosylation strategy with SLNs could be a promising approach in improving the delivery of DOX for cancer therapy.
•Adapalene (ADA) loaded tristearin, soya lecithin based solid lipid nanoparticles (SLNs-A) developed for spatial and temporal delivery to epidermis tissues.•SLNs shown spatial and temporal drug ...release behaviour.•SLNs formulations deliver significant amounts of ADA into the epidermal layer of skin that is necessary to produce desired effect.•The SLNs-A gel has shown adequate cohesiveness, fair extrudability and spreadability, as it is pre-requisite to sustain formulation.
Salient features such as controlled release, target ability, potential of penetration, improved physical stability, low cost compared to phospholipids, and ease of scaling-up makes solid lipid nanoparticles (SLNs) a viable alternative to liposomes for effective drug delivery. Adapalene (ADA) is a second generation retinoid effective in treating various dermatologic disorders such as Acne vulgaris with a few noticeable dose-mediated side effects. The present study was aimed at developing and characterizing ADA loaded SLNs for effective topical delivery. The formulated SLN system was characterized for particle size, poly dispersity index, entrapment efficiency and drug release properties. The resultant formulation (ADA loaded SLNs incorporated into carbopol hydrogel) was evaluated for in vitro drug release, skin permeation and bio-distribution, rheological behaviour, and texture profile analysis. The SLNs based ADA gel has shown its potential in targeting skin epidermal layer, and reducing systemic penetration. The developed system can avoid systemic uptake of ADA in skin layers, and can localize drug in skin epidermis as confirmed by rat skin model. Our results advocate potential of SLNs as a novel carrier for topical delivery of ADA in topical therapeutic approaches. This study open new avenues for drug delivery which better meets the need of anti-acne research.
•Glycone recognition is a futuristic platform for active targeting.•Galactose is widely explored carbohydrate ligand for targeted drug delivery.•Recent advances of various galactosylated ...nano-carriers for tumor-targeting are overviewed.•Galactosylated nano-carriers may be considered as safe and effective delivery system.
Galactosylated nanocarriers have recently emerged as viable and versatile tools to deliver drugs at an optimal rate specifically to their target tissues or cells, thus maximizing their therapeutic benefits while circumventing off-target effects. The abundance of lectin receptors on cell surfaces makes the galactosylated carriers suitable for the targeted delivery of bioactives. Additionally, tethering of galactose (GAL) to various carriers, including micelles, liposomes, and nanoparticles (NPs), might also be appropriate for drug delivery. Here, we review recent advances in the development of galactosylated nanocarriers for active tumor targeting. We also provide a brief overview of the targeting mechanisms and cell receptor theory involved in the ligand–receptor-mediated delivery of drug carriers.
Galactose-functionalized nanocarriers open new avenues for the design of highly effective multifunctional, targeted drug delivery systems.
•Microcapsules of β-carotene were prepared using casein and gum tragacanth.•Optimum pH of complex coacervation was found 4.35 with casein: gum tragacanth ratio of 2:1.•Encapsulation strongly ...increased the stability of micronutrients.•The release manners of β-carotene from microcapsules (MCs) showed an initial burst, followed by a slower sustained release.•Antioxidant activity of β-carotene was retained for longer time after microencapsulation.
Complex coacervation in casein/gum tragacanth (CAS/GT) mixtures was studied as a function of pH, initial protein to polysaccharide mixing ratio (Pr:Ps), total biopolymer concentration, core material load and ionic strength. This study is aimed at understanding how these parameters influence the coacervation kinetics, the coacervate yield, and entrapment efficiency. At a Pr:Ps=2:1, an optimum pH of complex coacervation was found 4.35, at which the intensity of electrostatic interaction was maximum. At these conditions, the phase separation occurred the fastest and the final coacervate yield and entrapment efficiency were the largest. Moreover, the developed β-carotene loaded microcapsules formulation was found to have particle size 159.71±2.16μm, coacervates yield 82.51±0.412%, entrapment efficiency 79.36±0.541%. Varying the Pr:Ps shifted the value of optimum pH. Electrostatic interaction and formation of coacervates was confirmed by Fourier Transform Infra Red (FTIR) spectra. Size and surface properties of coacervates were studied using Scanning Electron Microscopy (SEM). Entrapment of core material within the coacervates was confirmed by Confocal Laser Scanning Microscope (CLSM). The resultant formulation was evaluated for release study and antioxidant activity. Stability of encapsulated β-carotene was evaluated under three levels of temperature (5, 25 and 40°C) for 3 months. Encapsulation strongly increased the stability of micronutrients. Our results advocate potential of microcapsules as a novel carrier for the safeguard and sustained release of micronutrient.
