Stability Of Active Ingredients Research Articles

Microfluidic nanoparticle synthesis for oral solid dosage forms: A step toward clinical transition processes

Nanomedicine provides various opportunities for addressing medical challenges associated with drug bioavailability, stability, and efficacy. In particular, oral nanoparticles (NPs) represent an alternative strategy to enhance the solubility and stability of active ingredients through the gastrointestinal tract. The nanocarriers could be used for both local and systemic targeting, enabling controlled release of encapsulated drugs. This approach allows more efficient therapies.In this work, we aim to develop reliable oral solid dosage forms incorporating NPs produced by either one pot synthesis or continuous production, following protocols that yield highly consistent outcomes, promoting their technology transfer and clinical use.Microfluidics technology was selected to allow an automated and highly productive synthetic approach suitable for the highly throughput production.In particular, innovative systems, which combine advantage of NPs and solid dosage formulation, were designed, developed, and characterized demonstrating the possibility to obtaining oral administration. The resulting NPs were thus carried on oral dosage forms, i.e., pellets and minitablets. NPs resulted stable after dosage forms manufacturing, leading to confidence also on protection of encapsulated drugs. Indomethacin was used as a tracer to test biopharmaceutical behaviour.Anti-inflammatories or cytotoxic chemotherapeutics could be vehiculated leading to a breakthrough in the treatment of severe diseases allowing the oral administration of these drugs. We believe that the advancement achieved with the results of our work paves the way for the progression of nanoproducts into clinical transition processes.

Nanosponge: An Overview

The "Pharmaceutical Nanotechnology" subfield of pharmaceutical sciences, which is now in its infancy, offers new tools, prospects, and horizons with potential applications in the field of therapy and diagnostics of disease. Pharmaceutical nanotechnology consists of items that are nanosized and may be altered in many ways to enhance their properties. According to the administration method, the nanoporous particles are NSs that may entangle a wide variety of materials before being absorbed into a suitable formulation. They delay the drug's release in a regulated manner, stop the drug's protein from degrading, and disperse the drug where it is needed. They can move about the body, connect to the skin, and release the medicine at the intended target spot in a regulated and predictable way. They have excellent aqueous solubility, making them a carrier for medications with poor water solubility. When compared to other nanocarriers, they have greater drug loading capabilities. They are therefore appropriate for addressing issues with active ingredient stability, solubility, and delayed release. The main benefit of nanosponges of weakly water soluble medicines. They can function as biocatalysts in the administration of enzymes, proteins, vaccines, and antibodies and can administer medications via a variety of routes, including oral, topical, parental, etc.

Improving the stability of EGCG in the emulsified oil droplets by regulating the rheological properties of O/W emulsion

In this study, we encapsulated epigallocatechin gallate (EGCG) in emulsified oil droplets of protein-stabilized emulsions for the first time, with the participation of peppermint essential oil (PEO). Gum arabic (GA) and sodium caseinate (SC) were sufficiently crosslinked to construct the oil-water interface of the emulsion, improving the stability of EGCG in the emulsified oil droplets. When SC and 4 g/kg GA were mixed for 12 h before emulsification, the protein adsorption at the oil-water interface was significantly enhanced. Compared with the SC-stabilized emulsion, the retention of EGCG in the emulsion stabilized by mixing SC and 4 g/kg GA for 12 h increased about 2 and 33 times, respectively, after thermal treatment (30 min at 90 °C) and storage 10 weeks at 4 °C. Moreover, the emulsion stabilized by SC and 4 g/kg GA was resistant to the ionic strength of 0–0.6 mol/L and had predominantly elastic characteristics in the rheological properties. This indicates that the stability of active ingredients in emulsified oil droplets can be improved by regulating the rheological properties of the oil-in-water emulsion. The study is of great value for the efficient encapsulation and stability improvement of hydrophilic active ingredients in emulsified oil droplets based on emulsion systems.

Amphiphilic halloysite nanotube enclosing molybdenum oxide as nanoreactor for efficient desulfurization of model fuels

Hollow nanomaterials are regarded as the outstanding supports due to their confinement effect and stable carries, which can enhance the performance of the supported catalysts and even simplify the process. In this work, halloysite nanotubes (HNT) are chosen as the support due to their monoclinic tubular structures with two different surface compositions and charges. By a simple impregnation-calcination approach, MoOx is immobilized in the internal surface of HNT, then modify with organosilanes on the external surface of HNT to yield the amphiphilic Mo/HNT/S nanoreactor. The catalyst exhibits prominent activity for oxidative desulfurization in solvent-free system, the desulfurization rate of dibenzothiophene (DBT) reaches 100 % and the turnover frequency (TOF) value reaches 67.5 h−1 at 60 °C with 15 min, which is higher than most reported Mo-based catalysts. The hydrophobic surface enables the nanoreactor to be well dispersed in oil phase, and H2O2 solution in the hydrophilic cavity can extract DBT to form a concentrated microenvironment of the reactants and reactive oxygen species. The confinement function of the HNT nanoreactor can enhance the activity and stability of active ingredients (MoOx) over at least 5 cycles. Additionally, oxidation products can be retained in the hydrophilic lumen and completely separated from the model fuel. This amphiphilic catalytic system eliminates the following solvent extraction step in the ODS procedure. Thus, the catalyst is a promising candidate for large-scale industrial application.

Loss of Eicosapentaenoic Acid (EPA) after Retort Sterilization of the EPA-BCAA Fortified Complete Nutrition Drink

Retort sterilization is cost-effective for small-scale production of specialized nutrition products. However, the sensory properties and stability of active ingredients after sterilization remain undetermined. This study aimed to investigate the effect of retort on the existence of functional compounds and the sensory satisfaction of a fortified complete nutrition formula with branched-chain amino acids (BCAAs), and fish oil providing eicosapentaenoic acid (EPA). Changes in EPA and BCAA contents after retort were determined by using LC-MS/MS. Nutrient values, osmolality, rheology and sensory acceptance of the processed fortified and control formulas were compared. After retort, the fortified formula had an increase in all types of BCAAs but 30% loss of EPA (p = 0.001). The fortified formula had slightly higher protein and fiber contents, along with increased osmolality. It had higher viscosity and shear stress, but similar IDDSI level at 0. Among flavors tested, the fortified formula with Japanese rice flavor received the highest satisfaction scores with over 80% sensory acceptance. In conclusion, retort sterilization preserved BCAAs of the functional drink, but the addition of 30% fish oil was required to compensate for the EPA loss. The sterilized fortified formula with Japanese rice flavor was sensory acceptable.

Carbon nanotubes as control agents against the Khapra beetle, Trogoderma granarium Everts (Coleoptera: Dermestidae)

This may be attributed to the facts that nanotechnology has shown an excellent ability to control the release pattern of active ingredients of pesticides, so that it can achieve long-term functions more effectively, thus overcoming the problems of agricultural runoff and residual pesticide accumulation. In addition, Nanopesticides have shown greater solubility and stability of active ingredients, which can effectively control pests (Akhtar et al.,2020). In this study, the insecticidal relative toxicity of carbon nanotubes (CNTs) synthesized from seeds of Iraqi date palm Phoenix dactylifera L. using a chemical vapor deposition (CVD) method was investigated. These Nanoparticles were evaluated against adult and larvae of the Khapra beetle, Trogoderma granarium. The results indicated that CNTs (25, 50 and 100 ppm) caused mortality of the Khapra beetle under laboratory conditions. Additionally, the germination percentage of wheat, Triticum aestivum L. grains, has not been affected by the carbon nanotube treatments at 25-100 ppm. This study demonstrates the potential of CNTs as a technology for population control of T. granarium because of their toxicity to larvae and adults.

A Review on Multifunctional Excipients with Regulatory Considerations

The practice of multifunctional excipients is gaining more and more attention as it simplifies the process of drug formulation by substituting the necessity of using mixture of many excipients. The multifunctional excipients are the class of excipients which includes pre-–processed and co-processed excipients and it provides added functionalities to the formulation. Functionality of an excipient is a useful property which helps in manufacturing and improves quality as well as applicability of the material. Researchers have identified that single component excipients may not always give the required results during development and manufacturing of definite API, hence they are concentrating to develop multifunctional excipients which will have improved quality that will fulfil the requirements of the formulation experts in terms of cost. The cost of new excipient development is very high as it demands toxicity studies, hence the industry is now focusing on co-processing of approved materials. The demand for directly compressible co-processed excipients has also increased due to the availability of high-speed tableting machines, time saving in Abbreviated New Drug Application (ANDA), simplified validation and stability of active ingredients. The intention of this review article is to highlight applicability and increasing attention focusing the benefits of co-processed excipients. Their advantages over conventional blend of excipients include development methods, testing and also highlighting their regulatory consideration.

Comparative Stability of Two Anti-hyperpigmentation Agents: Kojic Acid as a Natural Metabolite and Its Di-Palmitate Ester, Under Oxidative Stress; Application to Pharmaceutical Formulation Design.

Purpose: Kojic acid (KA) a natural metabolite and its dipalmitate ester, kojic acid dipalmitate(Kadp) are both prescribed to treat skin hyperpigmentation. Stress test reveals the intrinsicstability of active ingredients and leads to selection of the suitable formulations. This researchevaluates the comparative stability of KA and its di-palmitate ester under liquid oxidative stress. Methods: The HPLC-UV/PDA method with a C18 column was utilized. Liquid oxidative stresswas induced using hydrogen peroxide (H2O2). Degradation was separately induced for eachdrug, and they were compared to each other. Results: Kadp degraded more rapidly in similar liquid oxidative stress conditions than KA did.The superior degradation model was the first order for both drugs based on the mean percentage error (MPE) values, indicating the dependency of the reaction rate on the initial concentrationof the reactive substance. Ring opening was proposed as the most possible theory for KA andKadp oxidative degradation. Conclusion: It is suggested to use KA instead of Kadp in less stable formulations, such asextemporaneous preparations. The incorporation of antioxidant excipients in Kadp formulationsis recommended for yielding better stability results. Formulating Kadp in the internal phase ofo/w emulsion formulations may protect this susceptive molecule from oxidative degradationduring the shelf life of the pharmaceutical preparation. Further studies are required to study theexact mechanism of the degradation process.

Study on the Nasogastric Tube Passage and the Stability of Active Ingredients in a Simple Suspension Method of Oral Drugs in Combination with Multiple Drugs

Study on the Nasogastric Tube Passage and the Stability of Active Ingredients in a Simple Suspension Method of Oral Drugs in Combination with Multiple Drugs

Lopinavir/ritonavir, a new galenic oral formulation from commercial solid form, fine-tuned by nuclear magnetic resonance spectroscopy

ObjectivesThe lopinavir/ritonavir combination is one of the first antiretroviral drugs to be used in the treatment of COVID-19. In incapacitated patients, such as those in intensive care, an oral liquid...

Development and characterisation of clobetasol propionate loaded Squarticles as a lipid nanocarrier for treatment of plaque psoriasis

Aim: The aim of this project is to improve the therapeutic effectiveness, permeation and retention of clobetasol propionate in sebaceous glands by reporting the use of Squarticles as lipidic nanosystem.Methods: Homogenisation method is used for the formulation of Squarticles (nanoemulgel) which was characterised on the basis of size, polydispersity index (PDI), viscosity, spreadability, DSC, % in vitro release, in vitro skin permeation deposition studies, and in vivo studies, scanning electron microscopic (SEM) and physical storage stability studies were done at different temperature conditions, i.e. 4 ± 2 °C, 25 ± 2 °C and 45 ± 2 °C for a period of 6 months for drug and formulation.Result: The morphological characterisation of prepared nanoemulsion shows small spherical shape and uniform size distribution as observed in the Scanning electron microscopic (SEM), having mean size (240.5 ± 9.2) and mean size distribution (0.282 ± 0.03) and zeta potential (−51.21). The drug release from optimised nanoemulsion (F2) in PBS (pH 5.5) was approximately 84.24 ± 1.35%, nanoemulgel formulations showed the release of 66.83 ± 2.05% while marketed gel showed the release of 57.67 ± 1.63% after 24 h. The cumulative percentage retention of clobetasol propionate loaded nanoemulgel was 63 ± 1.28% which was more than the marketed formulation (23.12% ±0.54). Physical stability studies show that formulation is more stable in cold condition. Further, the stability of active ingredient in gel formulation was determined using HPLC which shows around 15 ± 0.84% of loss in its activity.Conclusion: The present work has demonstrated the use of Squarticles as a novel carrier for treatment of plaque psoriasis by enhancing the better permeation, increasing skin retention, and enhances the effect of drug. The study also shows that the formulation is more stable in cold condition

Long-Term Antimicrobial Activity of Phage–Sugar Glasses is Closely Tied to the Processing Conditions

Bacteriophage-based antimicrobials have proven to be effective in the control of foodborne contaminants at various stages of the food production chain. Incorporating bacteriophages onto food-processing surfaces and food packaging can significantly impact food safety. One of the major roadblocks toward using phage as a natural antimicrobial/preservative in food packaging is phage sensitivity to desiccation. We recently developed a coating (film) composed of pullulan and trehalose that proved to be highly effective in preserving the antimicrobial activity of phage for more than 8 weeks. During this investigation, we realized that the conditions under which the films were formed and stored significantly affected the protective ability of these films toward bacteriophage antimicrobials, leading us to design a more in-depth investigation to identify and evaluate the major factors that affect the efficacy of these antimicrobial films. In this work, we report the outcome of a four-factor, two-level full-factorial randomized design of experiments, in which we examined the effects of four processing/storage factors on the short-term and long-term antimicrobial activity of phage-embedded pullulan/trehalose films. The drying method used to make the films and the storage humidity are the two factors that have the most significant impact on the long-term antimicrobial activity of pullulan/trehalose. The long-term viability of the bacteriophage (as measured by loss of titer) can be increased by over 1000-fold by using dry vacuum to form the films and then storing (for 28 days at room temperature) them in a closed container (tube) with low humidity in the headspace. The presence of divalent ions during the drying process and modification of the surface onto which the films were cast did not have a significant effect on long-term phage viability. Coatings, such as a pullulan/trehalose film, can help realize the promise of phage in the food industry. Insights in the control and stabilization of active ingredients in pullulan/trehalose films can also be applied to stabilization of viral vaccines and diagnostic bioassays.

Advances in Targeted Pesticides with Environmentally Responsive Controlled Release by Nanotechnology.

Pesticides are the basis for defending against major biological disasters and important for ensuring national food security. Biocompatible, biodegradable, intelligent, and responsive materials are currently an emerging area of interest in the field of efficient, safe, and green pesticide formulation. Using nanotechnology to design and prepare targeted pesticides with environmentally responsive controlled release via compound and chemical modifications has also shown great potential in creating novel formulations. In this review, special attention has been paid to intelligent pesticides with precise controlled release modes that can respond to micro-ecological environment changes such as light-sensitivity, thermo-sensitivity, humidity sensitivity, soil pH, and enzyme activity. Moreover, establishing intelligent and controlled pesticide release technologies using nanomaterials are reported. These technologies could increase pesticide-loading, improve the dispersibility and stability of active ingredients, and promote target ability.

The Application of 3D Printing in the Formulation of Multilayered Fast Dissolving Oral Films

Fast-dissolving oral films (FDFs) provide an alternative approach to increase consumer acceptance by advantage of rapid dissolution and administration without water. Usually, FDFs require taste-masking agents. However, inclusion of these excipients could make developing the formulation a challenging task. Hence, this work employed fused-deposition modeling three-dimensional printing to produce single-layered FDFs (SLFDFs), or multilayered FDFs (MLFDFs) films, with taste-masking layers being separated from drug layer. Filaments were prepared containing polyethylene oxide (PEO) with ibuprofen or paracetamol as model drugs at 60°C. Also, filaments were produced containing polyvinyl alcohol and paracetamol at 130°C. Furthermore, a filament was prepared containing PEO and strawberry powder for taste-masking layer. FDFs were printed at temperatures of 165°C (PEO) or 190°C (polyvinyl alcohol) with plain or mesh designs. High-performance liquid chromatography and mass spectroscopy analysis indicated active ingredient stability during film preparation process. SLFDFs had thicknesses as small as 197 ± 21 μm, and MLFDFs had thicknesses starting from 298 ± 15 μm. Depending on the formulation and design, mesh SLFDFs presented disintegration time as short as 42 ± 7 s, and this was 48 ± 5 s for mesh MLFDFs. SLFDFs showed drug content uniformity in the range of 106.0%-112.4%. In conclusion, this study provides proof-of-concept for the manufacturing of FDFs by using 3D printing.

IPNs from Cyclodextrin:Chitosan Antioxidants: Bonding, Bio-Adhesion, Antioxidant Capacity and Drug Release.

IPNs are unique “alloys” of cross-linked polymers in which at least one network is synthesized and/or cross-linked in the presence of the other. IPNs are also known as entanglements of polymer networks that are ideally held together only by permanent topological interactions. The objectives of this study are to evaluate novel chitosan-based functional drug delivery systems that can be successfully incorporated into “dual action bioactive tooth restorative materials”. These materials should be capable of inducing an improved wound healing prototype. The novel hydrogels will be investigated with respect to the antioxidant capacity of conventional antioxidants, such as resveratrol, β-carotene and propolis, as a designer drug delivery system, with the use of SEM imaging for the characterization of the surfaces, bio-adhesive property, antioxidant capacity, free radical defence, antioxidant, active ingredient stability and reactive features of novel materials. The additional benefit of the site-specific “functional restorative material” for use in dressings to deliver antibiotics to wound sites can provide tissue compatibility and reduced interference with wound healing. The materials were tested using an effective in vitro free radical generation model as functional additive prototypes for further development of “dual function restorative wound healing materials”. We quantified the effects of functional designer biomaterials on the dentin bond strength of a composite and evaluated the bio-adhesive capacity of the materials in the two separate “in vitro” systems. The added benefits of the chitosan/vitamin C/cyclodextrin (CD) host:guest complex-treated hydrogels involved a positive influence on the tetracycline release, increased dentin bond strength, as well as a demonstrated in vitro “built-in” free radical defence mechanism and, therefore, acting as a “proof of concept” for functional multi-dimensional restorative wound healing materials with a built-in free radical defence mechanism. Based on our results, we can conclude that the CD:chitosan-antioxidant-containing hydrogels are a suitable carrier for tetracycline to be slow-released. Within the limitations of the study design, chitosan-based hydrogels are suitable materials for functional restorative and wound healing applications in vitro. Cytotoxicity data are currently being evaluated in our laboratory.

Evaluation of stability and simultaneous determination of fimasartan and amlodipine by a HPLC method in combination tablets

A simple, rapid, accurate, precise and robust HPLC method was developed for the simultaneous determination of fimasartan and amlodipine in tablet dosage form. Furthermore, stability of active ingredients was evaluated under normal and stress conditions. The isocratic elution was accomplished by Nucleosil C18 column (250 mm × 4.6 mm, 5 μm) at 40 °C. The mobile phase consisted of acetonitrile and 0.02 M monopotassium phosphate buffer (pH 2.2) in the ratio of 50:50 (v/v) was eluted at 1.0 ml/min. The eluent was monitored by the UV detector for fimasartan and amlodipine at 237 nm for 8 min, detection time. The validation of HPLC method was carried out in accordance with the ICH guidelines.

Validation of data on the use of twin mix in minor oral surgery: comparative evaluation of efficacy of twin mix versus 2 % lignocaine with 1:200000 epinephrine based on power analysis and an UV spectrometry study for chemical stability of the mixture

There is convincing evidence supporting the addition of dexamethasone to lignocaine and its administration as an intra-space injection to achieve benefit of a single dose steroid after third molar surgery. This study was undertaken to validate the existing data on the use of twin mix in minor oral surgery based on power analysis, statistical sample size estimation and an ultraviolet (UV) spectrometry study for chemical stability of the mixture. A prospective, randomized, double-blind trial was designed to validate the pilot study on the efficacy of twin mix and 2% lignocaine with 1:200,000 epinephrine in the surgical removal of impacted mandibular third molars. Clinical parameters of anaesthetic latency, anaesthetic duration, efficacy of twin mix as an anaesthetic and post-operative patient discomfort were assessed. The stability of active ingredients in the solution was assessed using a double beam UV-visible spectrophotometery. The results of the study showed better post-operative outcome with administration of dexamethasone and lignocaine as an intra-space injection in decreasing the post-operative patient discomfort. The anaesthetic efficacy of the twin-mix admixture was found statistically similar to the control solution of 2% lignocaine with 1:200,000 epinephrine. The λmax recorded for dexamethasone and local anaesthetic individually was obtained with the twin-mix solution, which indicated no change in the active pharmacological compounds. Clinical anaesthetic efficacy of twin mix is comparable to 2% lignocaine with 1:200,000 epinephrine when administered in the pterygomandibular space with the additional advantage of a single prick co-administration of dexamethasone with local anaesthetic, lesser sting of the local anaesthetic injection, shorter anaesthetic latency, prolonged duration of the soft tissue anaesthesia and decrease in post-operative discomfort after the oral surgical procedure.

Comment Regarding the Stability of Active Ingredients in Long-Expired Prescription Medications—Reply

Comment Regarding the Stability of Active Ingredients in Long-Expired Prescription Medications—Reply

Comment Regarding the Stability of Active Ingredients in Long-Expired Prescription Medications

Comment Regarding the Stability of Active Ingredients in Long-Expired Prescription Medications

Stability of Active Ingredients in Long-Expired Prescription Medications

Stability of Active Ingredients in Long-Expired Prescription Medications