Excipient Concentration Research Articles

FORMULATION AND EVALUATION OF HERBAL TOOTHPASTE

The present study is concerned with the formulation and evaluation of herbal toothpaste, which contains various properties like tooth abrasives, tooth whitening, anti-caring, antibacterial, anti-inflammatory, desensitivity, etc. The herbal toothpaste was prepared using mango leaf extract and guava leaf extract as active ingredients, along with various excipients, which include calcium carbonate, sodium chloride, sodium lauryl sulphate, sodium benzoate, glycerine, camphor, honey and distilled water. The toothpaste was prepared by homogeneous mixing of all the excipients and the herbal extract. Four formulations were prepared using mango leaf extract as an active ingredient along with varying excipient concentrations, four formulations were prepared using guava leaf extract as an active ingredient along with varying excipient concentrations, and a polyherbal formulation consisting of four formulations containing both mango leaf extract and guava leaves extract as active ingredients along with varying excipient concentrations. The formulations were tested for various parameters such as homogeneity, abrasiveness, foamability, moisture content, Spreadability, extrudability, colour, PH, and antibacterial activity. The study concluded that polyherbal formulation showed best results and was found to be best among all batches. The polyherbal formulation, F4 showed was found to be best among all other formulations.

Comparison of oven drying and freeze drying methods for the production of fast melt films containing quetiapine fumarate

Background Quetiapine fumarate (QTP) is commonly prescribed for schizophrenic patient, typically available in tablet or oral suspension form, presenting challenges such as administration difficulties, fear of choking and distaste for its bitter taste. Fast melt films (FMF) offer an alternative dosage form with a simple development process, ease of administration and rapid drug absorption and action onset. Objective This study aims to prepare FMF with different formulations using solvent casting methods and to compare the effects of different drying methods, including oven drying and freeze drying, on the properties of the films. Methods Various formulations were created by manipulating polymer types (starch, hydroxypropyl methylcellulose (HPMC) and guar gum) at different concentrations, along with fixed concentrations of QTP and other excipients. Characterisation tests including surface morphology, weight, thickness, pH, tensile strength, elongation length, Young’s modulus, folding endurance and disintegration time were conducted. The optimal FMF formulation was identified and further evaluated for moisture and drug content, dissolution behaviour, accelerated stability, X-ray diffraction (XRD), and palatability. Results FMF containing 10 mg guar gum/film developed using oven drying emerged as the optimum choice, exhibiting desirable film appearance, ultra-thin thickness (0.453 ± 0.002 mm), appropriate pH for oral intake (pH 5.0), optimal moisture content of 11.810%, rapid disintegration (52.67 ± 1.53 seconds), high flexibility (folding endurance > 300 times) and lower Young’s modulus (1.308 ± 0.214). Conclusion Oven drying method has been proven to be favourable for developing FMF containing QTP, meeting all testing criteria and providing an alternative option for QTP prescription.

Comparison of in vitro screening methods for evaluating the effects of pharmaceutical excipients on membrane permeability

The effects of pharmaceutical excipients on intestinal drug absorption have been highlighted and careful excipient selection is required to develop biologically equivalent formulations. This study aimed to evaluate the effects of excipients on drug permeability and compare the characteristics of in vitro screening methods. Three in vitro models, the commercial precoated parallel artificial membrane permeability assay (PAMPA), PermeaPadTM, and Caco-2 monolayer, were used to evaluate the effects of 14 excipients on the permeability of several drugs with different biopharmaceutical classification system classes. Concentration-dependent effects were analyzed to distinguish non-specific effects. The permeability of low-permeability drugs was increased by excipients such as hydroxypropyl cellulose and povidone K30 in the precoated PAMPA model, whereas PermeaPadTM maintained membrane integrity at higher concentrations. Conversely, croscarmellose sodium and sodium lauryl sulfate (SLS) decreased the permeability of highly permeable drugs in both precoated PAMPA and PermeaPadTM assays in a concentration-dependent manner. In Caco-2 monolayer assays, most excipients showed minimal effects on drug permeability. However, SLS significantly reduces the permeability of highly permeable drugs at concentrations above the critical micelle concentration, thereby compromising the integrity of the cell monolayer. Our results suggested that most of excipients, except SLS, did not affect the membrane permeation of drugs at clinically used concentrations. The pre-coated PAMPA model demonstrated high sensitivity to excipient effects, making it suitable for conservative evaluation. The PermeaPadTM and Caco-2 models allowed assessment at higher excipient concentrations, with PermeaPadTM being particularly useful for excipients that cause toxicity in Caco-2 cells.

The influence of thermal radiation during microwave-assisted freeze-drying of pharmaceutical unit doses

New drying technologies for biologicals have recently been developed to accelerate the time-consuming batch freeze-drying (BFD) process. Among others, microwave-assisted freeze-drying (MFD) has been suggested as a faster and more effective drying technology. In this study, MFD cycles with the microwave radiation switched on and off were performed to assess the contribution of the microwave radiation to drying acceleration. It was found that thermal radiation emitted by the drying chamber walls was predominantly accelerating the drying of monodose placebos rather than microwave radiation. The combination of ultra-low chamber pressure, high thermal heat transfer and a short primary-to-secondary phase transition reduces drying times by more than 80 % compared to conventional BFD. In a second step, a design of experiment approach was used to assess the effect of thermal radiation versus microwave radiation and their combination, together with dosage properties such as fill volume and excipient concentration upon drying rate. The outcome showed the importance of high fill volume and high excipient concentration for an effective microwave contribution to the drying rate. Nevertheless, the drying acceleration for small pharmaceutical dosages with restricted solutes was mainly driven by thermal radiation rather than 2.45 GHz microwave radiation. The inability of ice to convert microwave energy into heat hampers the potential use of microwave freeze-drying for single-dose vaccines.

Fabrication and Characterization of Andrographolide-loaded Microsponges to Enhance Oral Bioavailability of Drug against Colon Cancer Using HT29 Cells

Background: The current research aimed to determine ways to improve the bioavailability of andrographolide (AGP) for use in colon cancer treatment by developing and evaluating microsponges loaded with the drug. Methods: Utilising the quasi-emulsion solvent diffusion approach, microsponges containing AGP were synthesised. A total of ten formulations were prepared using different concentrations of drug, polymer and other excipients. Particle size, shape, and differential scanning calorimetry (DSC) were used to characterise the microsponges that were created. To find out the rate at which the microsponges would expel their contents, researchers measured their release dynamics. In vitro anticancer activity of formulation was determined using HT29 cells Results: Results showed that the percentage yield of the formulations ranged from 10.85-41.03%. The highest drug concentration was achieved in formulation F8 with a particle size of 33.7 nm. SEM analysis demonstrated that the particles were round and possessed a rough and porous surface. Increasing the ratio of ethyl cellulose to AGP reduces surface roughness. The microsponge's DSC difractogram reveals prominent peaks at 18°, 24°, and 38° (2 θ) with reduced intensity, suggesting that the microsponges' crystalline character has diminished. In vitro drug release study showed 93.85% release upto 12 hours. Mathematical models showed normal release of the formulations with “n” values greater than 0.90 of all the formulations. Formulation F8 decreased the HT-29 cells' ability to survive. The percentage of cell cytotoxicity was 75.54 at 100μg/ml. Since AGP microsponges had a detrimental effect on the survival of colorectal cancer cells. Conclusion: It can be concluded from the study that prepared formulations possess anticancer properties against cancerous cells and can be used as an alternative anticancer drug.

Pulmonary Inhalation of Biotherapeutics: A Systematic Approach to Understanding the Effects of Atomisation Gas Flow Rate on Particle Physiochemical Properties and Retained Bioactivity.

The identification of spray-drying processing parameters capable of producing particles suitable for pulmonary inhalation with retained bioactivity underpins the development of inhalable biotherapeutics. Effective delivery of biopharmaceuticals via pulmonary delivery routes such as dry powder inhalation (DPI) requires developing techniques that engineer particles to well-defined target profiles while simultaneously minimising protein denaturation. This study examines the simultaneous effects of atomisation gas flow rate on particle properties and retained bioactivity for the model biopharmaceutical lysozyme. The results show that optimising the interplay between atomisation gas flow rate and excipient concentration enables the production of free-flowing powder with retained bioactivity approaching 100%, moisture content below 4%, and D50 < 4 µm, at yields exceeding 50%. The developed methodologies inform the future design of protein-specific spray-drying parameters for inhalable biotherapeutics.

Investigation of Groundnut Shell Powder as Potential Super Disintegrant in Chronotherapeutic Delivery of Sacubitril–valsartan

ABSTRACT Context: Chronotherapeutic delivery of antihypertensives plays a potential role in the treatment by providing a therapeutic amount of drug at the target site in the body. Sacubitril–valsartan (SV), an angiotensin receptor neprilysin inhibitor, has been indicated for the treatment of hypertension. The study explores the formulation and evaluation of compression-coated tablets (CCTs) of SV using a natural super disintegrant in the core tablet for chronotherapeutic drug delivery. Aim and Objective: The main objective of the current investigation is to study the applicability of groundnut shell powder (GSP) as super disintegrant and its role in chronotherapeutic drug delivery. Materials and Methods: Core tablets of SV were prepared using different concentrations of natural excipient (GSP) and compression coated. The CCT was evaluated for the postcompression tableting properties, in vitro drug release, Fourier transform infra red spectroscopy (FTIR), and stability studies and compared the disintegrating property with a synthetic excipient (crospovidone). Results: The results of the in vitro dissolution performance of core tablets indicated that the incorporation of GSP as a super disintegrant significantly reduced the disintegration time. Optimized core tablets were subjected to compression coating using a graded concentration of cellulose acetate phthalate as coating polymer and evaluated tableting properties and dissolution performance. Among all the formulations, CCT5 with 8% GSP in the core, coated with 300 mg coating polymer shown 6 h lag time followed by the rapid release of the drug within 1 h. Accelerated stability studies on optimized formulation revealed that there were no significant changes in the tableting parameters after storage indicating the stability of the formulation. Conclusion: The use of natural disintegrant in the core tablet offers a promising approach for rapid release of drug from CCT after a lag time of 6 h to achieve chronotherapy of SV.

Awareness, Practice, and Views of Pediatricians, General Physicians, and Pharmacists about Prescribing Off-label Medication in Pediatric Patients in Eastern Province, Saudi Arabia.

An off-label medication involves the use of an approved drug for an unapproved indication, population, route of administration, or dosage.The physiological state of children differs from that of adults, making the adult formulation potentially dangerous to children. Off-label prescribing is quite common in children due to challenges in the development of pediatric formulations. The current study was conducted to determine the awareness, practice, and views of pediatricians, general physicians, and pharmacists about prescribing Off-label medication to pediatric patients in Eastern Province, Saudi Arabia. A cross-sectional study based on a questionnaire was conducted among pediatricians, general physicians, and pharmacists (clinical and community) in Eastern Province, Saudi Arabia. Statistical analysis was conducted using the data exported from Google Forms (Mountain View, California, USA) and Microsoft Excel (Version 2016) and then exported into Statistical Package for Social Sciences (SPSS) version 26.0 (IBM, Inc., Armonk, NY, USA). Chi-square was deemed suitable. The level of significance was set at 0.05. Among the study participants, 53(35.09%) were pharmacists, followed by 24(15.89%) others, 22(14.565) pediatricians, 19(12.58%) other specialists, 17(11.25%) general physicians, and 16(10.59%) were clinical pharmacist. About 73(48.34%) described the definition of off-label correctly. About 114(75.49%) believed that parents and guardians must be informed about off-label medicine prescribed to their children. About 52(34.43%) had concerns about the safety of the medication, and 98(64.90%) believed they should be tested in pediatrics during clinical trials. Further, 97(64.23%) considered themselves not enough knowledgeable about off-label medications. The barriers reported by the participants were as follows: 89(58.945%) said lack of information resources, 71(47.01%) said lack of training, 56(37.08%) said lack of information on the safety of excipients used in pediatrics, 47(31.12%) said lack of formulary, 44(29.13%) said lack of guidelines, and 58(5.29%) said lack of information related to the safety of excipient concentration in pediatrics. The proportion of healthcare professionals who agreed that excipients in adult medication may be harmful to pediatrics was 103(68.21%). The drugs most often prescribed as off-label were paracetamol 54(21.68%), followed by Phenobarbital 35(14%), and Amoxicillin 33(13.25%). There are a considerable number of healthcare professionals unaware of the description of off-label medication. The majority have concerns over the safety and efficacy of the off-label drugs and believe that most frequently used off-label drugs in pediatrics must be tested in pediatrics during clinical trials. In addition, excipient safety data are of considerable importance to ensure off-label drug safety in pediatrics, who believe their knowledge is inadequate and need proper guidelines and training on this issue.

Formulation and Evaluation of Herbal Hair Serum

In daily life, there is a rising demand for cosmetics and are used by a large number of individuals annually. Humanity employs a variety of goods to accentuate elegance and attractiveness in order to appear youthful and endearing. Therefore, cosmetics are essential to human survival. Because of the perception that herbal cosmetics are safer and have fewer adverse effects, they are utilized extensively these days. One of the main bodily components that serve as a protective appendage is hair. The spreadability test and stability test results were all assessed. It was the development of a daily-use herbal hair serum is the main objective of this study. To achieve this, a range of herbs will be employed, and the ideal formulation will be determined by evaluating the cosmetic serum’s qualities. Three different cosmetic serum formulations (H1, H2, and H3) with different excipient concentrations have been developed. Physical properties, pH, homogeneity test, and viscosity ensured that every parameter fulfilled the norms and was in good condition. Herbal compositions have been shown to be useful in improving hair consistency.

Mucoadhesive Buccal Tablet Formulation of Azithromycin dihydrate for treatment of Upper Respiratory Tract Infection

The buccal drug delivery system is a versatile delivery system which can be designed for local or systemic effect. The objective of the study was to developed patient complacent tablet which can give sustain release of antibacterial agent for relief of upper respiratory tract infection. Azithromycin dihydrate is a semi-synthetic macrolide antibiotic widely used to prevent bacterial infections in the upper respiratory tract. The mucoadhesive buccal tablets of azithromycin dihydrate were formulated by varying concentrations of polymers (natural and synthetic), glidant and other excipients. The drug-excipient compatibility studies were carried out through DSC and FTIR studies. The selected excipients were found to be compatible. Further the dry blend of drug-excipients was evaluated for pre-compression properties. The prepared tablets were evaluated as per the general monograph for tablets of IP. The studies were also carried out to evaluate sustained release of the drug and mucoadhesivity of the tablets. A 23 level (2 level and 3 factors) factorial design was navigated to study the effect of natural, synthetic polymers and the glidant on mucoadhesive strength and percentage cumulative drug release at 8 hours. The responsive variables were analysed using ANOVA by Design-Expert version 12.0. It was concluded that these excipients significantly affected the response variables. The optimized tablet formulation was found to have an adequate mucoadhesion and a cumulative percentage release. The final product was performed for accelerated stability studies, optimized formulation was found to be stable at room temperature and accelerated temperature for three months.

How spray drying processing and solution composition can affect the mAbs stability in reconstituted solutions for subcutaneous injections. Part II: Exploring each protein stabilizer effect

Despite extensive research in spray drying of biopharmaceuticals, identifying the optimal formulation composition and process conditions to minimize the various stresses a biopharmaceutical undergoes during this drying process. The current study extends previous research on investigating how spray drying processing and solution composition can affect the stability of monoclonal antibodies (mAbs) in reconstituted solutions for subcutaneous injections. The decoupling process stresses on a model mAb (mAb-A) compared to the effect of coupled spray-drying stresses revealed that excipients and protein concentration had a more pronounced effect on stabilizing mAb-A against shear and thermal/dehydration stresses than spray drying operating conditions. These results prompted the continuation of the study, with the aim to investigate in greater depth the effect of mAb-A concentration in the formulation designated to spray-drying and then the effect of type and the concentration of individual excipients (sugars, amino acids and surfactants). The outcomes of this investigation suggest that a general increase in the concentration of excipients, particularly surfactants, correlates with a reduction in aggregation and turbidity observed in the reconstituted spray-dried mAb-A powders. These results, contribute to the identification of a suitable composition for a spray-dried mAb-A powder that ensures robust stability of the protein in reconstituted solutions intended for subcutaneous injection. This valuable insight has important implications for advancing the development of pharmaceutical formulations with enhanced stability and efficacy.

The Processing Space of the Spray-Dried Mannitol-Leucine System for Pulmonary Drug Delivery.

Designing spray-dried particles for inhalation aims at specific physicochemical properties including a respirable aerodynamic diameter and adequate powder dispersibility. Leucine, an amphiphilic amino acid, has been shown to aid in optimizing bulk powder properties. Mannitol, a model crystalline active and common bulking agent, was co-sprayed with leucine at several excipient ratios, ethanol/water ratios, and spray dryer outlet temperatures in order to experimentally probe the underlying particle formation mechanisms in this binary crystalline system. During the droplet drying of two crystallizing components, the material that nucleates first will preferentially enrich the surface. It is desired to have a completely crystalline leucine shell to improve powder properties, however, mannitol competes with leucine for the surface depending on excipient concentration and manufacturing parameters. The resulting particles were studied initially and at a two-month timepoint via solid state characterization, visual analysis, and particle size analysis in order to detect changes in bulk powder properties. It was determined that, similar to systems where only leucine can crystallize, initial leucine saturation in the formulation dictates powder characteristics.

Nanocrystals: A Multifaceted Regimen for Dermatological Ailments

AbstractSkin disorders are the most common apprehension worldwide among different regions of the world. Topical route of administration offers benefits over other routes such as avoidance of first‐pass metabolism, low dose, longer residence time, and absence of off‐target delivery. Skin serves as a mechanical barrier for therapeutic delivery with selectively permeable essential molecules. Considering the structural complexity of skin, delivery of therapeutics at targeted site requires sophisticated method such as nanotechnology‐assisted therapeutic delivery. The roadmap for combinatorial approach of nanotechnology and skin therapeutics has proven significant in clinical and marketed products. Currently, various pharmaceutical aids such as nanocrystal (NCs), nanoparticles, nanoemulsion, nano‐micelles, nano lipidic carriers, and hybrid nanocarriers are currently in market. Among all the other nanocarriers, nanocrystal offers precedence over other nanocarriers due to its facile method of preparation, reproducibility, low excipient concentration, and high therapeutic loading capacity. The recent literature data suggest the breakthrough evolution of NCs in topical therapeutic delivery. The outcome of these interventions envisages the applicability of NCs for delivering molecules with compromised physicochemical characteristics such as solubility, stability, toxicity, and bioavailability concerns.

A model-based performance analysis of integrated chromatography-ultrafilter separation systems for monoclonal antibody (mAb) manufacturing

Robust and accurate modelling of bioprocess systems offers the opportunity to visualise strategies for rapid-scale up of production platforms from benchtop to industrial scale, but few studies investigate how mechanistic and hybrid models can be used to design integrated bio-manufacturing. This is especially true for downstream purification technologies used to separate mAbs from culture by-products, e.g. host cell proteins. Polishing chromatography (cation-exchange mode) is commonly used to remove these by-products, but optimal bind and elution operation of these columns is complex. Ultrafiltration is typically applied in conjunction with diafiltration post-polishing chromatography in order to obtain suitable final product titers and excipient concentrations. This study presents a combination of dynamic models to probe batch polishing chromatography and ultrafiltration operating strategies achieving industrial specifications for recovery yield and mAb titer. A series of elution and filtration strategies are implemented, resulting in a total of 40 flowsheets explored. A steric mass action model with 7 pH-dependent parameters is employed to simulate scale-up polishing chromatography column behaviour. Moreover, a published gel layer ultrafiltration model based on Darcy’s law is implemented to purify the outlet of the polishing chromatography column. Strategies that are successful in achieving the target 90% recovery yield and 100 g L−1 concentration specifications are compared via a comprehensive analysis, to deduce the operational protocols which offer minimised salt consumption and pressure drop whilst respecting design criteria.

Preparation and Characterization of Theophylline Controlled Release Matrix System Incorporating Poloxamer 407, Stearyl Alcohol, and Hydroxypropyl Methylcellulose: A Novel Formulation and Development Study.

Theophylline (THN), a bronchodilator with potential applications in emerging conditions like COVID-19, requires a controlled-release delivery system due to its narrow therapeutic range and short half-life. This need is particularly crucial as some existing formulations demonstrate impaired functionality. This study aims to develop a new 12-h controlled-release matrix system (CRMS) in the form of a capsule to optimize dosing intervals. CRMSs were developed using varying proportions of poloxamer 407 (P-407), stearyl alcohol (STA), and hydroxypropyl methylcellulose (HPMC) through the fusion technique. Their in vitro dissolution profiles were then compared with an FDA-approved THN drug across different pH media. The candidate formulation underwent characterization using X-ray diffraction, scanning electron microscopy, Fourier transform infrared spectroscopy, differential scanning calorimetry, and thermogravimetric analysis. Additionally, a comprehensive stability study was conducted. In vitro studies showed that adjusting the concentrations of excipients effectively controlled drug release. Notably, the CRMS formulation 15 (CRMS-F15), which was composed of 30% P-407, 30% STA, and 10% HPMC, closely matched the 12 h controlled-release profile of an FDA-approved drug across various pH media. Characterization techniques verified the successful dispersion of the drug within the matrix. Furthermore, CRMS-F15 maintained a consistent controlled drug release and demonstrated stability under a range of storage conditions. The newly developed CRMS-F15 achieved a 12 h controlled release, comparable to its FDA-approved counterpart.

Formulation and Development of Tara Gum-mediated Tablets for Delivery of Anticancer Drugs

Abstract Background: Natural polysaccharide tara gum (TG) has been investigated for several biological uses. The current study involved the administration of imatinib, an anticancer model medication, via TG. Methods: Imatinib-modified release tablets were developed using a direct compression method with different concentrations of TG and other excipients. Compressed tablets were evaluated for physicochemical properties. Result: All formulations had an in vitro disintegration time ranging from 10–23 min. Among the formulations, F6 exhibited excellent extended-release behaviour with 72% release over 12 h. TG tablets were rich in phytoconstituents, including saponins, tannins, phenolics, flavonoids, carbohydrates, proteins, and amino acids. Conclusion: TG has potential in the drug delivery application of anticancer medications as a rate-retarding polymer.

Formulation optimization and evaluation of oromucosal in situ gel loaded with silver nanoparticles prepared by green biosynthesis

Treating oral diseases remains challenging as API is quickly washed out of the application site by saliva turnover and mouth movements. In situ gels are a class of application forms that present sol-gel transition's ability as a response to stimuli. Their tunable properties are provided using smart polymers responsible for stimuli sensitivity, often providing mucoadhesivity. In this study, antimicrobial in situ gels of thermosensitive and pH-sensitive polymers loaded with silver nanoparticles were prepared and evaluated. The nanoparticles were prepared by green synthesis using Agrimonia eupatoria L. extract. According to the data analysis, the in situ gel with the most promising profile contained 15 % of Pluronic® F-127, 0.25 % of methylcellulose, and 0.1 % of Noveon® AA-1. Pluronic® F-127 and methylcellulose significantly increased the viscosity of in situ gels at 37 °C and shear rates similar to speaking and swallowing. At 20 °C, a behavior close to a Newtonian fluid was observed while being easily injectable (injection force 13.455 ± 1.973 N). The viscosity of the formulation increased with temperature and reached 2962.77 ± 63.37 mPa·s (37 °C). A temperature increase led to increased adhesiveness and rigidity of the formulation. The critical sol-gel transition temperature at physiological pH was 32.65 ± 0.35 °C. 96.77 ± 3.26 % of Ag NPs were released by erosion and dissolution of the gel after 40 min. The determination of MIC showed effect against E. coli and S. aureus (0.0625 mM and 0.5000 mM, respectively). The relative inhibition zone diameter of the in situ gel was 73.32 ± 11.06 % compared to gentamicin sulfate. This work discusses the optimization of the formulation of novel antibacterial in situ gel for oromucosal delivery, analyses the impact of the concentration of excipients on the dependent variables, and suggests appropriate evaluation of the formulation in terms of its indication. This study offers a promising dosage form for local treatment of oral diseases.

Itraconazole Self-Nano Emusifying Drug Delivery System for Enhancement of Solubility

The main objective of formulation is to enhance the bioavailability of the drug within the body. Some of the challenging subjects associated with poorly water-soluble drugs concern solubility and bioavailability factors. To overcome these problems, new technologies, such as lipid-based drug delivery systems including micro or nano emulsifying drug delivery system, have obtained importance in recent years, due to their enhanced solubility and bioavailability in the gastrointestinal tract. Such systems are solubilized within the lipid excipients or mixed with oils or surfactants/co-solvents to facilitate the solubility and absorption rate, which can enhance the bioavailability of the targeted drug. The research was targeted to develop a self-Nano Emulsifying drug delivery system (SNEDDS) for oral bioavailability enhancement of BCS II antifungal drug Itraconazole. Nano Emulsions are consignment methods that improve the solubility and distribution of lipid medicines to the intended areas. SNEDDS of Itraconazole were developed using Castor oil, Tween 20 as surfactant and PEG 200 as co-surfactant. SNEDDS formulation can be obtained through phase diagram approach. Pseudo Ternary phase diagrams were constructed, using Chemix software, to optimize the concentrations of excipients. Thermodynamic stability studies were satisfactory. Robustness to dilution did not exhibit phase separation and drug precipitation. The Among 4 formulations, B1F3 formulation showed more than 95% of drug content and were considered superior and subjected to droplet size analysis and zeta potential measurement. Droplet size ranged from 120 nm to 505 nm. The Nano size was obtained for formulation. The zeta-potential results indicated the range -35 mV. Based on all evaluation tests, formulation B2F3 was chosen as the best. Thus, this self-Nano Emulsifying drug delivery system should be an effective oral dosage form for improving oral bioavailability of lipophilic drug Itraconazole.

Process development of inhalation powders containing simvastatin loaded liposomes using spray drying technology

The development of an inhalation powder (IP) for cancer therapy is desired to improve the therapeutic response and patient compliance. The latest studies highlighted that statins, a class of drugs used in hypercholesterolemia, can have anticancer and antiinflammatory properties. Therefore, the aim of the study was to develop an IP containing liposomes loaded with simvastatin using spray drying technology, as well as to investigate the influence of formulation factors on the quality attributes of the IP by means of experimental design. Results highlighted that the composition of liposomes, namely type of phospholipid and cholesterol concentration, highly influences the quality attributes of IP, and the use of optimal concentrations of excipients, i.e. D-mannitol and L-leucine, is essential to preserve the characteristics of liposomes throughout the spray drying process. The in vitro characterization of the optimal IP formulation revealed that the total percentage of released drug is higher from the IP formulation compared to the powder of active substance (53.38 vs. 42.76%) over a period of six hours, and 39.67% of dry particles have a size less than 5 µm, making them suitable for inhalation. As a conclusion, spray drying technology can be effectively used in the development and preparation of IP containing liposomes.

Screening of solubilization potential of various green excipients for case of hydrophobic antituberculous thioacetazone

The present study is aimed at solving the problem of poor solubility of the antituberculosis drug thioacetazone (TAZ), the use of which, despite its effectiveness, is limited by toxicity and requires a reduction of the therapeutic dose. Such representatives of "green chemistry" as a deep eutectic solvent based on choline chloride with urea, native and modified cyclodextrins (β-CD and HP-β-CD) and biocompatible polymers (PVP and PEG) were used as solubilizing agents. DES and modified HP-β-CD proved to be the most effective, improving water solubility of TAZ by 106 and 24 times, respectively. β-CD and polymers showed a weak solubilizing potential, demonstrating the ineffectiveness of their application to reduce the hydrophobicity of the drug. In addition, the effect of temperature and concentration of excipients in an aqueous medium on drug dissolution was studied. The thermodynamic aspects of the dissolution and complex formation processes of in the selected systems are also characterized.