Development Of Formulations Research Articles

Postprandial nutrient dynamics and their implications for formulated feed development for the ornate spiny lobster (Panulirus ornatus)

AbstractCrustacean feeding morphology and postprandial nutrient processing is a highly size‐selective procedure. The digestive system of lobsters is predicated on grinding feed to a fine particle size before digestion. Therefore, fine pregrinding of raw materials may bypass the need for extensive grinding in the proventriculus and expedite digestive and absorptive processes. Panulirus ornatus juveniles (N = 56) were allocated to four feed groups (n = 14). Groups A, B and C were fed nutritionally identical feeds featuring raw materials ground to 1000 µm (Feed A), 500 µm (Feed B) and 200 µm (Feed C) while the fourth group (Group S) acted as a 24‐h nonfeeding baseline control group. Sequential postprandial haemolymph extractions were performed at 0.5, 1, 1.5, 2, 3.5, 5.5 and 24 h across treatment groups. Haemolymph samples were assessed and analysed for brix (%), total proteins (g L–1), glucose (mmol L–1) and cholesterol (mmol L–1). Brix was found to have significant positive correlations with all the haemolymph biochemical properties while no significant correlations were identified between individual lobster size and haemolymph properties. Analysis of deviance applied to mixed effects models did not identify significant differences in haemolymph properties across feed groups. Trends identified here are indicative of diurnal rhythm patterns, likely orchestrated by the release of the crustacean hyperglycaemic hormone (CHH) when anticipating a meal. Additionally, the use of brix values, may not be optimal for identifying postprandial trends, yet could remain a valid indicator of longer‐term nutritional status.

REVOLUTIONIZING DRUG DELIVERY INNOVATION: LEVERAGING AI-DRIVEN CHATBOTS FOR ENHANCED EFFICIENCY

This study aims to delineate the pivotal role of ChatGPT, an Artificial intelligence-driven (AI) language model, in revolutionizing drug delivery research within the pharmaceutical sciences domain. The investigation adopted a structured approach involving systematic literature exploration across databases such as PubMed, ScienceDirect, IEEE Xplore, and Google Scholar. A selection criterion emphasizing peer-reviewed articles, conference proceedings, patents, and seminal texts highlights the integration of AI-driven chatbots, specifically ChatGPT, into various facets of drug delivery research and development. ChatGPT exhibits multifaceted contributions to drug delivery innovation, streamlining drug formulation optimization, predictive modeling, regulatory compliance, and fostering patient-centric approaches. Real-world case studies have underscored its efficacy in expediting drug development timelines and enhancing research efficiency. This paper delves into the diverse applications of ChatGPT, showcasing its potential across drug delivery systems. It elucidates its capabilities in accelerating research phases, facilitating formulation development, predictive modeling for efficacy and safety, and simplifying regulatory compliance. This discussion outlines the transformative impact of ChatGPT in reshaping drug delivery methodologies. In conclusion, ChatGPT, an AI-driven chatbot, has emerged as a transformative tool in pharmaceutical research. Their integration expedites drug development pipelines, ensures effective drug delivery solutions, and augments healthcare advancements. Embracing AI tools such as ChatGPT has become pivotal in evolving drug delivery methodologies for global patient welfare.

In Vivo Pharmacokinetic Study of Polygonatum cyrtonema Polysaccharide DPC1 after Oral and Intraperitoneal Administration.

(1) Background: Polygonatum cyrtonema is a medicinal plant, and its polysaccharides are used for immunomodulation and the treatment of hyperglycemia. Investigation of the tissue distribution and pharmacokinetics of P. cyrtonema polysaccharide can further elucidate its pharmacological mechanisms. (2) Methods: A fluorescence-labeling approach using rhodamine B (RhB) as a fluorescent molecular probe was used for the quantitative assessment of the polysaccharide from dried P. cyrtonema (DPC1) samples, and the pharmacokinetics and tissue distribution of DPC1 were evaluated in mice after intraperitoneal or oral administration. (3) Results: DPC1 was successfully labeled with RhB, showing degrees of fluorescence labeling at 0.453% and 0.568% as determined by the ultraviolet and enzyme marker methods, respectively. DPC1-RhB was rapidly absorbed into the bloodstream after oral and intraperitoneal administration. Pharmacokinetic characteristics showed that oral administration and intraperitoneal administration were consistent with the features of a two-compartment model. (4) Conclusion: After administration, DPC1-RhB was primarily distributed in the tissues of the heart, spleen, and lung, indicating that the drug has a targeted effect on these tissues. Overall, the findings provide a comprehensive reference for the in vivo distribution of DPC1, together with a foundation for further elucidation of its pharmacological mechanisms and the development and application of DPC1 formulations.

Development and Evaluation of Two-Phase Gel Formulations for Enhanced Delivery of Active Ingredients: Sodium Diclofenac and Camphor.

The formulation of biphasic gels as potential semi-solid carriers for hydrophilic and lipophilic active substances is promising for the development of pharmaceutical preparations. The aim of this study was to design a stable bigel composition and to determine the influence of the organogel/hydrogel ratio on the gel's physical-chemical and structural-mechanical properties. The investigated compositions of organogel/hydrogel remained stable at ratios ranging from 5/95 to 40/60. After texture and microstructure analysis, bigels with 20/80 and 25/75 ratios were selected as carriers for the active ingredients, sodium diclofenac and camphor, for use as topical preparations for the treatment of muscle-joint inflammation and pain. Although other researchers have published data on the preparation and evaluation of bigels, there are no scientific results on the development of a two-phase gel with our proposed combination of APIs. Sodium diclofenac release was found to be higher when combined with camphor, which revealed the advantages of the biphasic formulation. The pseudoplastic behavior, thixotropy, and thermal stability of flow of the studied bigel samples was investigated by rheological analysis. Ongoing stability studies confirmed the minimal 6-month period.

Development and Characterization of Multi-Nutrient Formulations for Organic Farming

The study was to develop multi-nutrient formulations for organic farming containing all the essential macro and micronutrients. The experimental design selected was completely randomized design with 8 treatments and 3 replications. The experiment was conducted in the Department of Soil Science and Agricultural Chemistry, College of Agriculture, Vellayani, Kerala between Jan 2021-May 2021. Multi-nutrient formulations were developed using various organic nutrient sources like blood meal, soybean meal, rock phosphate, steamed bone meal, potassium sulfate, langbeinite, epsom salt, and borax permitted by National Programme for Organic Production. Formulations were prepared by mixing nutrient sources considering the nutrient requirement of nendran banana (N:P2O5:K2O @ 300:115:450 g plant-1) and the soil fertility status. The formulations were characterized for their physical, chemical and biochemical properties. On the basis of character analysis and principal component analysis the formulation F1 containing blood meal, rock phosphate, potassium sulfate, epsom salt and borax was found superior to other formulations. This was followed by F3 which contains blood meal, steamed bone meal, potassium sulfate, epsom salt and borax. Formulation F1 had 3.73 g cm-3 bulk density, 2.67% moisture content, 6.5 pH, 3.23 dSm-1 EC, 29.43% OC, 7.21% N, 2.71% P, 10.78% K, 5.98% Ca, 0.35% Mg, 4.45% S, 1174.11 mg kg-1 Fe, 4.53 mg kg-1 Mn, 13.55 mg kg-1 Zn, 8.65 mg kg-1 Cu and 93.67 mg kg-1 B. It also contained 45.04% crude protein, 2.95% humic acid and 3.55% fulvic acid. The formulation F3 had 7.47 pH, 3.37 dSm-1 EC, 28.34% OC, 7.11% N, 2.68% P, 10.68% K, 2.05% Ca, 0.32% Mg, 4.37% S, 1163.41 mg kg-1 Fe, 4.87 mg kg-1 Mn, 14.52 mg kg-1 Zn, 9.05 mg kg-1 Cu and 96.33 mg kg-1 B. Hence multi-nutrient formulation F1 based on its nutrient supplying capacity can be recommended as a nutrient source for organic farming.

Formulation Development and Evaluation of Ubidecarenone Chewable Tablet

Background: Coenzyme Q10 has a role in mitochondrial transport system and can be utilized as a supplement in migraine prevention. This study's objective is to assess Coenzyme Q10's effectiveness when used in conjunction with conventional medications to prevent migraines. Adding 300mg of coenzyme Q10 each day to prescription medications, while another group of patients continued receiving standard care. Over the course of a three-month treatment period, data on attack frequency, headache pain intensity, monthly migraine days, and associated symptoms like nausea, vomiting, phonophobia, and photophobia were analyses. Ubidecarenone, a medicinal component. The goal is to produce Ubidecarenone in a 300 mg chew-able tablet form. In vitro release studies and organoleptic properties, such as taste and flavour, will be evaluated. investigations in the early stages, tests for medicine excipient compatibility, and analyses of the water content Quality Assurance for the Process Hausner's Ratio, Bulk Density, Tapped Density, Comprehensibility Index, and Angle of Repose for calculating derived properties for medications and mixtures. ingredients that have been optimised for their concentrations, such as tastes, sweeteners, disintegrants, wetting agents, glidants, and lubricants. putting the best possible ingredients together to make a chew able pill. Evaluation of chewable tablets for post compression parameters including uniformity of weight, thickness, hardness, brittleness, friability, dissolution, assay, and in vitro drug release properties. An evaluation of the optimised batch's palatability is required. The intention is to create chewable tablets of ubidecarenone. Method: The wet granulation method is used to make chewable tablets of ubidecarenone. Mannitol is used as a diluent, crospovidone as a disintegrant agent, sodium starch as a disintegrate agent, saccharin sodium as a sucrose sweetener, orange flavour, peppermint oil as a flouring agent, and colloidal silicon dioxide as a gliding. The Ubidecarenone (300 mg) is one of the best first-line treatments for migraine prevention.

Drug Polymorphism: An Important Pre-formulation Tool in the Formulation Development of a Dosage Form

Abstract: Polymorphism permits solids to have two or multiple crystal structures with varying orientations or conformations, and polymorph drug dissolution and solubility vary. Polymorphism influences drug efficacy, bioavailability and toxicity. Various parameters can regulate polymorph crystallization, including supersaturation phase, temperature, stirring rate, solvent addition rate, seed crystal, additives and pH. To characterize and monitor polymorphs, various analytical approaches are available, including powder X-Ray diffraction / X-Ray diffraction (PXRD/XRD), also called as Gold Standard method, differential scanning calorimetry (DSC), Infrared spectroscopy (IR), and microscopical studies. To prevent polymorphic change during production, distribution, and storage, formulation with the most stable form in the marketed product is considered. In addition, by monitoring each phase of raw material processing, polymorphisms can be controlled during dosage form manufacturing. The objective of this review is to provide concise information on drug polymorphism, their characterization process, their effect on the stability of dosage forms, factors controlling polymorphism in the crystallization process, some case studies on polymorphs, control of polymorphism during the formulation of successful dosage forms and some of the regulatory considerations regarding polymorphs. Various databases like Pubmed/Medline, Google Scholar and Web of Science of all English language articles were searched, and relevant information was collected regarding the importance of polymorphism in formulation development. From a vast literature survey, it was found that polymorphism is a very important tool in a pre-formulation study that provides information about the fate of a drug molecule in its journey. From the present study, it was concluded that the polymorphism property of a drug should be taken into consideration at the pre-formulation stage since it is a very important tool for the formulation of a successful dosage form with stability and efficacy.

The Nanotech Potential of Curcumin in Pharmaceuticals: An Overview.

It is safe to use Curcumin as a cosmetic and therapeutic ingredient in pharmaceutical products. For the uses mentioned above and for fundamental research, it is essential to obtain pure Curcumin from plant sources. There is a requirement for effective extraction and purification techniques that adhere to green chemistry standards for efficiency improvement, process safety, and environmental friendliness. Several outstanding studies have looked into the extraction and purification of Curcumin. This review thoroughly covers the currently available curcumin extraction, synthesis, and transformation techniques. Additionally, Curcumin's poor solubility and low absorption in the human body have limited its potential for pharmaceutical use. However, recent developments in novel curcumin formulations utilizing nanotechnology delivery methods have provided new approaches to transport and maximize the human body's curcumin absorption efficiency. In this review, we explore the various curcumin nanoformulations and the potential medicinal uses of nano curcumin. Additionally, we review the necessary future research directions to recommend Curcumin as an excellent therapeutic candidate.

Development of succinate-based analogues and formulations against influenza virus infection

Development of succinate-based analogues and formulations against influenza virus infection

Recent developments in the use of nanocrystals to improve bioavailability of APIs.

Nanocrystals refer to materials with at least one dimension smaller than 100 nm, composing of atoms arranged in single crystals or polycrystals. Nanocrystals have significant research value as they offer unique advantages over conventional pharmaceutical formulations, such as high bioavailability, enhanced targeting selectivity and controlled release ability and are therefore suitable for the delivery of a wide range of drugs such as insoluble drugs, antitumor drugs and genetic drugs with broad application prospects. In recent years, research on nanocrystals has been progressively refined and new products have been launched or entered the clinical phase of studies. However, issues such as safety and stability still stand that need to be addressed for further development of nanocrystal formulations, and significant gaps do exist in research in various fields in this pharmaceutical arena. This paper presents a systematic overview of the advanced development of nanocrystals, ranging from the preparation approaches of nanocrystals with which the bioavailability of poorly water-soluble drugs is improved, critical properties of nanocrystals and associated characterization techniques, the recent development of nanocrystals with different administration routes, the advantages and associated limitations of nanocrystal formulations, the mechanisms of physical instability, and the enhanced dissolution performance, to the future perspectives, with a final view to shed more light on the future development of nanocrystals as a means of optimizing the bioavailability of drug candidates. This article is categorized under: Therapeutic Approaches and Drug Discovery > Emerging Technologies Nanotechnology Approaches to Biology > Nanoscale Systems in Biology.

A Patent Review on Cardiotoxicity of Anticancerous Drugs.

Chemotherapy-induced cardiotoxicity is an increasing concern and it is critical to avoid heart dysfunction induced by medications used in various cancers. Dysregulated cardiomyocyte homeostasis is a critical phenomenon of drug-induced cardiotoxicity, which hinders the cardiac tissue's natural physiological function. Drug-induced cardiotoxicity is responsible for various heart disorders such as myocardial infarction, myocardial hypertrophy, and arrhythmia, among others. Chronic cardiac stress due to drug toxicity restricts the usage of cancer medications. Anticancer medications can cause a variety of adverse effects, especially cardiovascular toxicity. This review is focused on anticancerous drugs anthracyclines, trastuzumab, nonsteroidal anti-inflammatory medications (NSAIDs), and immune checkpoint inhibitors (ICI) and associated pathways attributed to the drug-induced cardiotoxicity. Several factors responsible for enhanced cardiotoxicity are age, gender specificity, diseased conditions, and therapy are also discussed. The review also highlighted the patents assigned for different methodologies involved in the assessment and reducing cardiotoxicity. Recent advancements where the usage of trastuzumab and bevacizumab have caused cardiac dysfunction and their effects alone or in combination on cardiac cells are explained. Extensive research on patents associated with protection against cardiotoxicity has shown that chemicals like bis(dioxopiperazine)s and manganese compounds were cardioprotective when combined with other selected anticancerous drugs. Numerous patents are associated with drug-induced toxicity, prevention, and diagnosis, that may aid in understanding the current issues and developing novel therapies with safer cardiovascular outcomes. Also, the advancements in technology and research going on are yet to be explored to overcome the present issue of cardiotoxicity with the development of new drug formulations.

Intranasal Drug Delivery of Antiviral Agents - A Revisit and Way Forward

Abstract: Even to this date, oral drug delivery in the form of tablets, capsules, and syrups is considered as the most accepted one. However, oral delivery as a methodology requires that the active molecules and their formulations are water-soluble. Nasal drug delivery is characterized by ease of permeability through the epithelial mucosa, low enzyme activity, and a wide range of immunocompetent cells. For the transfer of drugs and active molecules through the nasal route, it is often essential to resort to nanodelivery methods, such as liposomes, microspheres, nanoemulsions, and so on. The use of nanodelivery vehicles has become more important in the modern context of viral infections, including those of the respiratory tract. Nanoformulations are developed in the form of nasal gels, sprays, drops, rinses, etc. Nanoformulations of antigens, vaccine and immune adjuvants, and antivirals are now gaining importance. There are promising reports on nanoparticles of metals, metal oxides, polymers, and so on that have the potential to detect and inhibit viruses by themselves. This review looks into the nasal nanoformulations in detail and provides an insight into how their efficacy can be improved. To overcome known drawbacks, such as degradation and active mucociliary clearance by antigenpresenting cells at the site of administration, polymers, such as PEG, are incorporated in the nanoformulation. Polymeric systems also provide better tunability of physicochemical properties. The mechanism of nasal spray-based drug delivery systems is also discussed in this paper. The review, thus, provides a detailed insight into the way forward for the development of nasal formulations.

Quantifying the bitter masking effect of drug-cyclodextrin complexation: NMR-ROESY mixing time approach

Taste, especially unpleasant taste, can be key for patient compliance. In the formulation development process, drug-cyclodextrin (CD) inclusion complexes are often used to improve the solubility of a drug and/or mask its bitterness. This study aimed to evaluate the bitter masking effect of CDs on different drugs using NMR-ROESY analysis, human sensory tests, and e-tongue measurements. The strength of inclusion complex formation between drugs and CDs was investigated by NMR-ROSEY, and these results were compared to human sensory test results. In the sensory test, participants identified which drug-CD inclusion complexes were not bitter. NMR-ROSEY results aligned with the sensory tests; short magnetization transfer times corresponded to masked bitterness. The electrical tongue was not able to detect the taste of any of the drug-CD inclusion complexes. Additionally, we used NMR-ROSEY to determine which drug-CD inclusion complex formed in a system with multiple drug substances present. This research offers valuable insights into the bitter masking effect of CDs on different drugs and presents a comprehensive evaluation approach using various methods. This knowledge has significant implications for the pharmaceutical industry, clinical practice, and patient care, contributing to improved patient compliance and satisfaction with bitter medications.

Enhancing Drug Delivery Precision: Development and Optimization of Nanoparticle-Based Formulations for Targeted Therapy in Preclinical Models

In recent years, the utilization of nanoparticles has proliferated across a wide spectrum of clinical domains. Nanoparticles have been engineered to surmount the constraints associated with free therapeutics and negotiate biological barriers—systemic, microenvironmental, and cellular—that exhibit heterogeneity across diverse patient cohorts and diseases. Mitigating this patient heterogeneity has also been facilitated through precision therapeutics, where tailored interventions have augmented therapeutic effectiveness. Nonetheless, current nanoparticle development predominantly emphasizes the refinement of delivery platforms with a uniform approach. As lipid-based, polymeric, and inorganic nanoparticles undergo increasingly nuanced engineering, there arises the potential for tailoring them to drug delivery in a more personalized manner, ushering in the era of precision medicine. In this Review, we deliberate on sophisticated nanoparticle designs employed in both generalized and precision applications, offering insights into their potential for enhancing precision therapies. We concentrate on advancements in nanoparticle design that surmount heterogeneous barriers to delivery, positing that intelligent nanoparticle design can enhance efficacy in broad delivery applications while facilitating customized designs for precision applications, thereby ultimately enhancing overall patient outcomes.

Reliable particle sizing in vaccine formulations using advanced dynamic light scattering

Understanding the impact of lipid nanoparticle size on immunogenicity represents an important step for enabling the rapid development of novel vaccines against known or emergent diseases. Dynamic light scattering, also known as quasi-elastic light scattering or photon correlation spectroscopy, has established itself as an optimal analytical method to determine particle size due to its in-situ approach and fast measurements. However, its application to many systems of industrial relevance has been hindered due to artifacts arising from multiple scattering. Result interpretation becomes severely compromised depending on the concentration of the system and the size of the particles. In this context, strong sample dilution is often required, bringing additional uncertainties to the formulation development process. Here, we show how advanced dynamic light scattering technology can filter out multiple scattering from the signal and yield fully accurate sizing measurements regardless of the sample concentration. We illustrate this in a comparative study with standard dynamic light scattering using polystyrene beads as model suspension as well as a concentrated commercial lipid nanoparticle adjuvant (AddaVax™).

Combined green analytical principles and quality by design for ultraperformance liquid chromatography analytical method development, the characterization and in-silico toxicity prediction of Ixazomib degradation products using mass spectrometry

Ixazomib citrate (IC) is the first oral selective proteosome inhibitor for treating multiple myeloma. IC is prone to degradation due to its oxidative deboronation and the amide bond, affecting patient health, drug quality, and efficacy. The stability of IC is crucial during drug development as it guides the inherent stability of the molecule, its degradation pathways, packing materials, and formulation development. Following the International Conference on Harmonization (ICH) Q1A (R2) and Q1B, a stability study were performed for both solution and solid-state stress studies. Under oxidative and alkaline conditions, 3 degradation products (DPs) were identified, separated, and method-validated according to ICH Q2 (R1) guidelines. From the Design Expert statistical tool, the Central Composite Design was used to optimize the final analytical method conditions, where the p-values for the model are < 0.05%. Green analytical chemistry has significantly reduced the use of hazardous organic solvents without losing chromatographic performance. The green separation and quantification of DPs and IC on Ultra Performance Liquid Chromatography (UPLC) using an Inert-Sustain C8 (50×3.0) mm 2.0 µm column with gradient elution using 10 mM ammonium acetate buffer (pH 5.0) and ethanol at a flow rate of 0.5 mL/min and detection at 230 nm. The results of green assessment tools like GAPI, AGREE, and Analytical eco-scale found that the method is excellent for the greenness of utilizing ethanol as a solvent, shorter runtime, and lesser waste. The method was validated as per ICH Q2 guidelines, and the results found it is sensitive, precise, accurate, robust, and linear for its intended use. The method is suitable for quantifying IC and its DPs from 2.0 to 150 µg/mL with R2 values of 0.9996 with a detection limit of 1.0 µg/mL. The plausible degradation structures and pathways of DPs were outlined using tandem mass spectra employed on LC-QTOF-MS/MS in both ESI positive and negative modes. The mechanistic explanation for establishing DPs was explained in detail. The ADMET Predictor™ software predicted the physicochemical and ADMET properties. The toxicity profile reveals that DP2 and DP3 are teratogenic, while D1 and D3 show phospholipidosis.

Impact of milling on the nutrients and anti-nutrients in browntop millet (Urochloa ramosa) and its milled fractions: evaluation of their flour functionality.

Browntop millet has gained popularity in recent years owing to its nutritional superiority and health benefits. However, the usage of browntop millet flours as ingredients in composite flours and functional foods is constrained due to a lack of information regarding the grain composition and its flour functionality. Therefore, the distribution of nutrients, anti-nutrients in browntop millet milled fractions and their flour functionality was evaluated in comparison to whole grain flour. Bran fraction comprised the highest protein (13.7%) and fat contents (27%) among other fractions. Pearling of dehulled grains considerably reduced phytic acid, saponins and flatulence-causing oligosaccharides in pearled grain flours. Besides, this led to the enrichment of soluble fibre, minerals, phenolics and trypsin inhibitors in bran fraction. Milling also impacted flour functionality. Despite its lower water holding ability, dehulled grain flour exhibited significantly higher oil absorption capacity than whole grain flour due to the removal of fibre-rich hull fraction. Although emulsion (45.2%) and foaming capacities (12.5%) were superior in bran flour, foam stability was greater in pearled grain flours. These findings suggest the potential utilisation of browntop millet milled flours as ingredients in the development of distinct food formulations and as partial substitutes to wheat flour in confectionary and bakery products. © 2024 Society of Chemical Industry.

Formulation and Evaluation of Topical Delivery Diosgenin Emulgel for Diabetic Wounds

A variety of cellular processes work together in a highly coordinated manner to facilitate a complex and dynamic process of wound healing ensuring the efficient restoration of injured tissue. Diosgenin, a plant sterol saponin is primarily found in various plants. The aim of this research was to create an emulgel containing Diosgenin and examine its effects on wound healing in diabetic rats with excision wounds. Histopathological findings further supported the efficacy of the emulgel and results indicate that the application of Diosgenin Emulgel (DE) shows an effective approach for healing of diabetic wounds. The objective of the research stands to explore the possibility of formulation development and wound-healing capabilities of DE. The study evaluated the wound healing effects of the DE in Streptozotocin-induced (STZ) (55 mg/kg) given by intraperitoneal route diabetes and control group. The emulgel was topically applied to assess its effectiveness in promoting wound healing. The application of DE on the rat wounds resulted in a notable wound closure within a 21-day period and significant epithelization was observed with p &lt; 0.001. The study concluded that the formulation demonstrated remarkable effectiveness in promoting the functional recovery of diabetic wounds.

Development and Validation of a Chromatographic Method for Ibrutinib Determination in Human and Porcine Skin

Ibrutinib (IBR) is a tyrosine kinase inhibitor investigated for treating solid and non-solid tumors. Considering the advantages that a topical application of IBR could generate in terms of dose reduction and side effects in skin cancer treatment, this paper presents a simple and selective HPLC method for determining IBR concentration in in vitro skin permeation studies to support the development of topical formulations. The method uses a reversed-phase C18 column and a mobile phase composed of acetonitrile and 0.01 mol/L phosphoric acid at pH 3.5 (35:65 v/v), flowing at 1.0 mL/min. The oven temperature was set at 35 °C, the injection volume was 20 μL, and UV drug detection was performed at 259 nm. The validation procedure certified that this method was selective for IBR determination even when extracted from human or porcine skin matrices. The method was linear over a range of 0.2 to 15.0 μg/mL, precise, robust, and accurate, with recovery rates from the skin layers higher than 89.5 ± 5.9% for the porcine skin and higher than 92.0 ± 0.2% for the human skin. The limits of detection and quantification were 0.01 and 0.02 μg/mL, respectively. The method showed, therefore, to be adequate for use in further skin permeation studies employing IBR topical formulations.

Development of microencapsulated grape juice powders using black 'Isabel' grape peel pectin and application in jelly formulation with enhanced in vitro bioaccessibility of anthocyanins.

In this study, pigmented pectin (grape pectin, GP) was extracted from the peels of black Isabel grapes. This highly methoxylated GP was composed mainly of galacturonic acid, arabinose, and other neutral monosaccharides. Its red color was ascribed to the anthocyanin content, and the main contribution was from malvidin-3-O-glucoside. To improve the yield and color properties of spray-dried Isabel grape juice powders, maltodextrin (MD) was substituted with this colored GP. When 25% of MD was substituted with GP, the powder yield increased from 46.0% to 60.4%, but it decreased to 21% when the substitution was 40%. GP inclusion increased the encapsulation efficiency of total anthocyanin in powders from 55.70% to 88.66%. When this spray-dried grape juice powder containing GP was utilized in a jelly recipe (4%-10%), a higher level of inclusion yielded stronger and more brittle jellies. When the jellies containing varying amounts of GP were subjected to in vitro digestion, the formulation with a higher amount of GP yielded a higher recovery of anthocyanins. In addition to being utilized as a carrier agent for spray-drying applications, this pigmented GP can also be tailored for a variety of applications, such as the development of pH-sensitive edible films and functional beverage formulations.