Formulation Components Research Articles

Evaluation of Physicochemical, Microstructure Parameters (Q3) and Performance Attributes of Commercial Ketoprofen Gels.

In vitro methods for quality and equivalence assessment of semi-solid products applied to the skin have increasingly garnered attention because in vivo bioequivalence studies is high cost, complexity, and time-consuming. Regulatory authorities established draft guidelines that outline a modular framework demanding qualitative, quantitative, microstructure and product performance equivalence to support generic products. In line with these guidelines, our study aimed to evaluate the relationship between microstructure and performance attributes in both originator and generic semi-solid products applied to the skin. In this context, reference and three generics of ketoprofen gel were selected as models for semi-solid formulations. Microstructure of all products was assessed regarding pH, specific gravity, drying rate, formulation rheology and potential drug polymorphism. Additionally, performance attributes of products were evaluated using in vitro release testing and in vitro permeation testing. Polymorphism and drying rate data showed no significant difference in microstructure of ketoprofen gels. All tested products exhibited pseudo-plastic flow behavior with thixotropic characteristic. However, differences in pH, specific gravity and viscosity values at low shear stress were observed between reference product and generic products, according to EMA guidance. Although IVRT outcomes did not entirely align with Q3 attributes, IVRT results for reference product versus Generic Product-I and Generic Product-II met the acceptance limits according to FDA guidance, which differs from EMA's assessment. Furthermore, in vitro release rate results were consistent with IVPT data. Consequently, it can be concluded that microstructure of semi-solid products applied to the skin may not consistently correlate with performance attributes due to various alternations influenced by manufacturing process parameters and/or formulation components.

Solid Lipid Nanoparticles as an Innovative Lipidic Drug Delivery System.

In order to overcome some of the drawbacks of traditional formulations, increasing emphasis has recently been paid to lipid-based drug delivery systems. Solid lipid nanoparticles (SLNs) are among these delivery methods, and they hold promise because of their simplicity in production, capacity to scale up, biocompatibility, and biodegradability of formulation components. Other benefits could be connected to a particular route of administration or the makeup of the ingredients being placed into these delivery systems. This article aims to review the significance of solid lipid nanocarriers, their benefits and drawbacks, as well as their types, compositions, methods of preparation, mechanisms of drug release, characterization, routes of administration, and applications in a variety of delivery systems with a focus on their efficacy.

Solid lipid nanoparticles for transdermal delivery of curcumin: Optimization using factorial design and in vitro characterization

This study aimed to design and optimize Curcumin (CUR) loaded solid lipid nanoparticle (SLNs) transdermal formulations by nano emulsion template method. A 3 factor, 2 level Box-Behnken design was used to evaluate the effect of three independent variables viz., Amount of Span 60 (X1), Tween 60 (X2) and Stearyl alcohol (X3) on dependent variables viz., Particle size (Y1), entrapment efficiency (Y2) and zeta potential (Y3). Optimization study signifies that amount of formulation components viz., Span 60, Tween 60 and Stearyl alcohol influence the vesicle size, entrapment efficiency and Zeta potential. The numerical optimization was validated within the design space. The OP-CUR-SLNs exhibited good entrapment efficiency and particle size. Further the OP-CUR-SLNs loaded transdermal carbopol gel shows good in vitro drug release and better ex vivo permeation than the plain CUR loaded gel, which concludes CUR-SLNs considered to be a successful topical transdermal drug delivery system and provide a sustained release of encapsulated drug. Furthermore, CUR-SLNs loaded carbopol gel considered to be non-irritant and safe to be applied on the skin for the intended period of time.

New PPARα Agonist A190-Loaded Microemulsion for Chemotherapy-Induced Peripheral Neuropathy.

Chemotherapy-induced peripheral neuropathy (CIPN) is a serious side effect of anticancer agents with limited effective preventive or therapeutic interventions. Although fenofibrate, a peroxisome proliferator-activated receptor-alpha (PPARα) agonist, has demonstrated neuroprotective and analgesic properties, its clinical utility is hindered by low receptor affinity, poor subtype selectivity, and suboptimal bioavailability. A190, a highly selective and potent nonfibrate PPARα agonist, offers a promising alternative but is limited by poor aqueous solubility, resulting in reduced oral bioavailability and therapeutic efficacy. To address these limitations, an optimized oil-in-water (o/w) microemulsion formulation was developed using Box-Behnken design to enhance the solubility and intestinal permeability of A190. The A190 microemulsion exhibited physical stability with a droplet size of approximately 100 nm and a drug loading efficiency of greater than 95%. The effective and apparent permeability of A190 from the microemulsion was significantly higher compared to that of free A190 dispersion, respectively. Additionally, no significant impact on the cell viability was observed, indicating less toxicity and a good biocompatibility of the formulation components. The oral bioavailability of A190 microemulsion was approximately 5-fold higher compared to A190 dispersion, demonstrating the microemulsion's potential to greatly enhance the oral bioavailability of hydrophobic drugs. Furthermore, our findings reveal that orally administered A190 microemulsion effectively reduced CIPN-induced mechanical hypersensitivity, likely mediated through PPARα activation. A190 microemulsion was found to be equally effective at reducing the chronic inflammatory complete Freund's adjuvant-induced pain. These results underscore A190s potential as a nonopioid therapeutic candidate, utilizing a novel microemulsion formulation for the management of chemotherapy-induced neuropathic pain and chronic inflammatory pain.

Nano-biopesticide formulation comprising of silver nanoparticles anchored to Ocimum sanctum: a sustainable approach to pest control in jute farming

The jute hairy caterpillar, Spilosoma obliqua (Lepidoptera: Erebidae) is considered as one of the major threats to jute cultivation. The best eco-friendly methods to combat these jute pests involve administration of nano-biopesticides, as a successful alternative to the toxic chemicals. In this study, a nano-biopesticide formulation containing green synthesized silver nanoparticles (Ag NPs) using Ocimum sanctum leaf extract has been proposed. The characterization studies confirmed significant interactions between the Ag NPs and bioactive components in the nano-biopesticide formulation. The comparative analysis of the aforementioned larval mortality showed better responses in the nano-biopesticide formulation rather than the crude (pure) leaf extract. The LC50 values were calculated both for the nano-biopesticide formulation and pure extract after 24, 48 and 72 h of treatment. The nano-biopesticide formulation was found to exhibit the lowest and much promising LC50 value of 93.21 ppm, 23.38 ppm, 5.96 ppm relative to that of LC50 values of 1590.74 ppm, 459.30 ppm, 102.68 ppm respectively for the crude leaf extract. The synergistic interactions between the components in the nano-biopesticide formulation can be associated with its greater effectiveness as a promising toxicant to the larvae of the jute caterpillar compared to the mere leaf extract, thereby, demonstrating a greener and safer method for effective pest management.

ИССЛЕДОВАНИЕ ВЛИЯНИЯ БЕЛКОВОГО ПРОФИЛЯ НА КРИСТАЛЛООБРАЗОВАНИЕ В МОДЕЛЬНЫХ МОЛОЧНЫХ СИСТЕМАХ С ПРОМЕЖУТОЧНОЙ ВЛАЖНОСТЬЮ

The purpose of research is to study the influence of the protein profile of model dairy systems with intermediate moisture content on the process of crystal formation of milk sugar (lactose). Research objectives: selection of formulation components for compiling a protein profile and study of its influence on the process of formation and growth of lactose crystals in model systems during storage. The objects of research were model systems with targeted adjustment of pH values in each of them, imitating skimmed condensed milk with sugar, in which the complete or partial replacement of the protein phase with whey proteins was carried out through the use of dry whey protein concentrate, dry hydrolyzed whey protein (obtained in native or denaturing conditions), dry cheese whey. Studies of microstructural changes in consistency were carried out using the method for determining the size of lactose crystals according to GOST 29245-91. It has been established that a change in the protein profile towards an increase in the content of native and transformed whey proteins in model systems led to a slowdown in the process of lactose crystal formation. At the same time, hydrolyzed whey proteins had a higher degree of crystal growth restriction. The complete replacement of the protein phase with dry whey protein concentrate and dry cheese whey contributed to the intensive growth of crystals at their initial minimum average size (relative to other samples). However, after 14 days of storage, the average crystal size in this model system was comparable to the rest of the samples (including the control), except for the sample using hydrolyzed whey proteins. Regularities of the influence of the active acidity of the medium on the size of the crystals were also revealed. A decrease in pH from 6.2 to 5.6 leads to the formation of lactose crystals of a smaller average size by 1.9–3.3 times.

Bridging Experimentation and Computation: OMSP for Advanced Acrylate Characterization and Digital Photoresin Design in Vat Photopolymerization.

Vat photopolymerization (VPP) is an additive manufacturing method that requires the design of photocurable resins to act as feedstock and binder for the printing of parts, both monolithic and composite. The design of a suitable photoresin is costly and time-consuming. The development of one formulation requires the consumption of kilograms of costly materials, weeks of printing and performance testing, as well as the need to have developers with the expertise and knowledge of the materials used, making the development process cost thousands. This paper presents a new characterization methodology for acrylates that allows for the computerization of the photoresin formulation development process, reducing the timescale to less than a week. Okoruwa Maximum Saturation Potential (OMSP) is a methodology that uses attenuated total reflection (ATR-FTIR) to study the functional group of acrylates, assigning numerical outputs to characterize monomers, oligomers and formulations, allowing for more precise distinguishment between materials. It utilizes the principles of Gaussian normal distribution for the storage, recall, and computerization of acrylate data and formulation design without the need to database numerous files of spectral data to an average coefficient of determination (R2) of 0.97. The same characterization method can be used to define the potential reactivity of acrylate formulations without knowing the formulation components, something not possible when using properties such as functionality. This allows for modifications to be made to unknown formulations without prior knowledge of their contents. Validation studies were performed to define the boundaries of the operation of OMSP and assess the methodology's reliability as a characterization tool. OMSP can confidently detect changes caused by the presence of various acrylates made to the photoresin system and distinguish between acrylates of the same viscosity and functionality. OMSP can compare digitally mixed formulations to physically mixed formulations and provides a high degree of accuracy (R2 of 0.9406 to 0.9964), highlighting the future potential for building foundations for artificial intelligence in VPP; the streamlining of photoresin formulation design; and transforming the way acrylates are characterized, selected, and used.

Optimization of Carrier-Based Dry Powder Inhaler Performance: A Review.

Dry powder inhalers (DPI's) are becoming increasingly popular due to growing interest in pulmonary drug delivery and their performance is the net result of a series of processes carried out during the formulation development and manufacturing process such as excipient selection, blending, milling, filling, and spray drying. To reach the small airways of the deep lung, the active pharmaceutical ingredients (API) particles need to have an aerodynamic diameter of 1-5 μm to avoid impaction and particle sedimentation in the upper respiratory tract, and due to this small particle size, the powder becomes highly cohesive resulting in poor flow. Therefore, API is usually blended with a coarse carrier to improve flowability, and due to its large size, it is more fluidizable than the micronized drug. Carrier-based DPI formulations usually consist of micronized drugs, a coarse carrier, and additional components, such as micronized lactose and force control agents, including magnesium stearate or leucine. Additionally, the manufacturing process of DPIs relies heavily on powder processing technologies, such as the micronization of API, blending, and powder filling. The aerosol performance of a DPI is significantly affected by the selection of formulation components and the processing of the formulation and, therefore, it is crucial to evaluate these parameters. This review will discuss different factors influencing the aerosol performance of carrier-based DPIs, including formulation components, device considerations, and manufacturing parameters. Additionally, novel technologies pertaining to the optimization of DPI performance are also discussed.

Making Waves: Formulation components used in agriculture may serve as important precursors for nitrogenous disinfection byproducts.

N-Nitrosamines, many of which are carcinogenic, mutagenic, and teratogenic, are disinfection byproducts (DBPs) formed from the reaction of chloramine with nitrogenous organic compounds during water disinfection. The identification of major nitrosamine precursors is important to understand and prevent nitrosamine formation. In this analysis, we propose that efforts to identify nitrosamine precursors must look beyond conventionally evaluated active agent chemicals to consider inert or inactive chemicals as potentially relevant precursors. Using agricultural chemicals applied in the US as an example, we demonstrate that amines widely used as inactive agents in herbicide formulations (i.e., dimethylamine [DMA], a known N-nitrosamine precursor) are potentially much more important than active agent herbicides previously evaluated as potential nitrosamine precursors (i.e., the herbicides diuron or trifluralin). Accounting for use rates and nitrosamine yields, amines used in herbicide formulations represent potential nitrosamine precursor inputs to the environment that are similar in magnitude to recognized precursors like the pharmaceuticals ranitidine and metformin. Because the amounts of amines used as inert agents in herbicide formulations have increased dramatically over recent decades, particularly in certain US regions, we suggest that identification of potential nitrosamine precursors should consider variation in the inputs of both active and inactive agents over time, as well as geographical variation in use that may alter the relative importance of specific precursors in certain locations.

Antibiotic Stewardship in Silkworms: Navigating the Pros and Cons

To safeguard against microbial diseases and maintain optimal silk yields, the sericulture industry relies on antibiotics to promote the health, well-being, and vitality of silkworms (Bombyx mori). Antibiotics are commonly incorporated into synthetic diets for rearing silkworms or included as key components in bed disinfectant formulations. The silkworm-rearing industry’s reliance on antibiotics has led to concerns about the development of antibiotic-resistant bacteria. Previous research has uncovered a dual role for antibiotics: not only do they prevent disease, but they also promote silkworm growth by reshaping the gut microbiome and enhancing nutrient absorption, highlighting the need for judicious use. Therefore, there is a critical need for prudent management and further exploration of alternative growth-promoting strategies to minimize resistance risks. This study investigates the relationship between antibiotic administration and silkworm growth, shedding light on the mechanisms underlying antibiotic-induced effects and assessing the risk of antimicrobial resistance (AMR) emergence and dissemination.

Solid dispersion of alectinib HCl: preclinical evaluation for improving bioavailability and establishing an IVIVC model

Objective Alectinib HCl (ALB-HCl) is a BCS class IV molecule with low solubility and low oral bioavailability. Owing to its low bioavailability, a high dose of ALB-HCl is recommended with food to meet clinical efficacy. Thus, there is a need for a delivery system to overcome the bioavailability concerns. Methods Three solid dispersion (SD) formulations (I, II, and III) were evaluated for in-vitro dissolution and in-vivo pharmacokinetics (PK) study in Wistar rats. An in-vitro and in-vivo correlation (IVIVC) model was developed to establish a relationship between in-vitro dissolution data and in-vivo PK data. The formulations were subjected to stability studies. Results All formulations showed enhanced dissolution in all the media except Formulation I in FaSSIF media. In-vivo PK studies displayed that Formulation I was inferior to API alone. Formulations II and III (amorphous SD [ASD]) exhibited two-fold higher Cmax and AUC0–last than API alone. Level A IVIVC model was established for Cmax and AUC0–last with an acceptable % prediction error (PE). When evaluated for external predictability, the model was found validated for Cmax (% PE <10%), however, it was inconclusive for AUC0–last (%PE −14.03). Stability studies showed ASD formulations were stable during storage. Conclusion A stable ASD formulation of ALB-HCl was successfully developed with improved bioavailability. Developing an IVIVC model can act as a surrogate to predict in-vivo performance. The selection of formulation components in ASD shall be rationalized for bioavailability and stability before clinical evaluation.

Harnessing the potential of 2-methyl imidazolium dihydrogen phosphate as a protein stabilizer: Assessing its toxicity and impact on aggregation, structural integrity, and functional efficacy of monoclonal antibodies

The development of safe and effective biotherapeutics faces challenges due to protein aggregation. These aggregates, formed due to various stress factors, can lead to irreversible changes and increase the risk of immunogenicity and off-target binding. Ionic liquids (ILs) have recently gained significant attention due to their potential in stabilizing proteins and enzymes. In this investigation, we have assessed the thermal stability of bevacizumab (BmAb), in presence of 2-methyl imidazolium dihydrogen phosphate (2- MIDHP), both alone and in combination with other formulation excipients. SEC, DLS, FFF-MALS and AUC were used to study the protective effect of 2-MIDHP on BmAb aggregation. CD and fluorescence spectroscopy were used to evaluate the impact of 2-MIDHP on structural changes in BmAb, while SPR was used to assess the binding activity in the presence and absence of 2-MIDHP. Subsequently, a cell viability assay (MTT) was conducted to evaluate potential toxic effects of 2-MIDHP with BmAb. Overall, our findings suggested the potential of 2-MIDHP in enhancing the stability of BmAb without any negative impact on its structural and binding activity, and its compatibility with other formulation components, thus indicating its promising prospects for the development of improved biotherapeutics.

Unveiling the Therapeutic Mechanisms of Taraxasterol from Dandelion in Endometriosis: Network Pharmacology and Cellular Insights.

AimsEndometriosis is a chronic inflammatory disease. The current treatment options in clinical practice mainly include hormonal therapy and surgical intervention. However, hormonal therapy is associated with serious side effects, and surgical treatment often leads to a high recurrence rate. Dandelion, a commonly used traditional Chinese medicine, has played a significant role in the treatment of endometriosis due to its notable efficacy and minimal side effects as a component of compound formulations. The purpose of this study is to investigate the molecular mechanisms of Taraxasterol, the main component of dandelion, in the treatment of endometriosis. Materials and methodsThis study employed network pharmacology to screen potential targets associated with Taraxasterol in the treatment of endometriosis. Subsequently, molecular docking was performed to preliminarily validate the core targets. Furthermore, GO and KEGG enrichment analyses were conducted to identify potential signaling pathways related to the treatment. The mechanisms underlying the therapeutic effects of Taraxasterol on endometriosis were further validated through in vitro cell experiments, including Western blotting, colony formation assays, scratch assays, and CCK-8 assays. ResultsA total of 148 potential targets of Taraxasterol were selected through screening on a prediction website, along with 1,180 disease targets and 71 overlapping targets. Subsequently, the overlapping targets were imported into the STRING database to construct a protein-protein interaction (PPI) network, which was visualized using Cytoscape 3.7. Ten key targets were identified from the network, and preliminary validation was performed through molecular docking of these ten targets. Additionally, GO and KEGG analyses were conducted on the overlapping targets, resulting in the identification of the top 10 enriched GO terms and the top 20 KEGG pathways, which were subsequently visualized. Finally, cellular experiments demonstrated that taraxasterol inhibits the proliferation and migration of ectopic endometrial cells through the PI3K/Akt/mTOR pathway, while promoting apoptosis. ConclusionsOur study investigated the potential mechanisms underlying the therapeutic effects of Taraxacum officinale (dandelion) on endometriosis. Through network pharmacology and in vitro cellular experiments, we revealed that Taraxasterol, a bioactive compound present in dandelion, can inhibit the proliferation and migration of endometrial ectopic cells and promote apoptosis through the PI3K/Akt/mTOR pathway.

Fabrication and In Vivo Evaluation of In Situ pH-Sensitive Hydrogel of Sonidegib-Invasomes via Intratumoral Delivery for Basal Cell Skin Cancer Management.

Basal cell skin cancer (BCSC) develops when skin cells proliferate uncontrollably. Sonidegib (SDB) is a therapeutic option for the treatment of BCSC by inhibiting hedgehog signaling. The problems with SDB's low solubility, poor bioavailability, resistance, poor targeting, and first-pass action make it less effective when taken orally. This investigation set out to design an intratumoral in situ pH-sensitive hydrogel of SDB-invasomes (IPHS-INV) that can effectively treat BCSC by improving SDB's bioavailability, sustainability, targeting, and efficacy while also reducing its resistance and undesirable side effects. Numerous S-INV formulations were developed using Box-Behnken Design Expert and tested before settling on the optimum S-INV formulation. An experimental 7, 12-dimethylbenzanthracene (DMBA) carcinoma rat model was used for in vivo studies of the IPHS-INV formulation after it was combined with chitosan. Phospholipids (1.72% w/w), cholesterol (0.15% w/w), ethanol (1% v/v), and cineole (1.5% v/v) were shown to be the optimal components in the SDB-invasome formulation. The IPHS-INV formulation outperformed the permeation and bioavailability of free SDB by 7.14 and 6 times, respectively, and sustained its release by 57.41%. The IPHS-INV formulation showed a decrease in tumor volume of 99.05% and a reduction of hypercellular tumors, indicating its anti-cancer activity. The intratumoral IPHS-INV formulation maintained a higher concentration of SDB in tumors, indicating its targeting activity. These findings support the use of the intratumoral IPHS-INV formulation as an effective strategy for the treatment of BCSC.

Identification and Quantitation of Signature Constituents of Dant‐Kanti, a Herbo‐Dental Formulation Using UHPLC, HPTLC, and GC–MS, and its Anti‐Inflammatory Effects on Porphyromonas gingivalis Lipopolysaccharide‐Induced Human Macrophages

ABSTRACTA herbo‐dental formulation, Dant‐Kanti natural toothpaste consists of 13 potent medicinal herbs. The present study aims to comprehensively identify the signature phytometabolites present in Dant‐Kanti natural toothpaste using high‐performance thin layer chromatography (HPTLC), ultra‐high‐performance liquid chromatography (UHPLC), and gas chromatography–mass spectrometry (GC–MS) methods. Among the identified phytometabolites, gallic acid, piperine, and anethole, were quantified by UHPLC, whereas camphor, menthol, thymol, and eugenol were quantified using GC–MS. An inductively coupled plasma‐mass spectrometry was used to estimate the mineral contents in Dant‐Kanti natural toothpaste. To the best of our knowledge, these studies are the first‐ever to identify all the signature components in an herbal dental formulation. These developed and validated methodologies were then used across 25 distinct batches of Dant‐Kanti natural toothpaste, in oder to ascertain the consistency and homogeneity. Both the UHPLC, and GC–MS methods used in this study were validated as per ICH Q2 (R1) guidelines, and were found to be suitable, linear (r &gt; 0.99), and precise. In the cell‐biological study, Dant‐Kanti natural toothpaste showed a concentration‐dependent reduction in proinflammatory cytokine release, in human macrophages induced with Porphyromonas gingivalis lipopolysaccharide. This robust study methodology, validation, and results provide valuable insights into the complex composition of Dant‐Kanti natural toothpaste, and contribute to the understanding of its potential oral health benefits.

Formulation components influence on the structural and mechanical characteristics of the minced meat system

The main requirement for washed minced fish is the ability to form a structure, but the technochemical and especially organoleptic properties of such minced meat require adjustment and improvement. The purpose of the research is to develop recipes for a basic structured product and study additional ingredients that contribute to the creation of products with a balanced amino acid composition. In the basic product, the norms for adding chicken eggs, starch, and fat components that do not reduce the moisture-holding capacity, ultimate shear stress, gel strength and en sure the preservation of the structure-forming ability of the product have been experimentally established. It is recommended to add starch in an amount of no more than 5%, eggs 2–3%, as well as the combined use of vegetable oil and lard in a ratio of 3 and 7%, respectively. Corrective additives have been proposed to obtain a product with a complete amino acid composition and acceptable organoleptic characteristics. In these additives, the indicators of the biological value of protein and the balance of the amino acid composition have been studied using the method of N.N. Calculation of the utility coefficients of individual amino acids showed that in all products they are less than one. The digestibility is close to 90%, the lowest is for chum salmon and pink salmon mince – 79.32%, the highest is for chicken eggs – 91.64%. All selected products are recommended for use to adjust the balance of the amino acid com position by creating two-component product compositions of the "shell – filling" or "sandwich" type..

A Rheological Study of Creams and Gels Containing N-Acetyl Glucosamine in Nanoparticle Form: The Advantages of a Bioengineered Strategy for Natural Anti-Inflammatory Substance Vehiculation

Topical formulations that include natural active compounds to treat inflamed and aching skin are favored by patients. Small local producers use commercial creams and gels to which they add compounds, often with criteria based more on trends than scientific evidence, to obtain products to treat inflamed joints or skin. Based on our previous studies that demonstrated the anti-inflammatory and analgesic effects of Harpagophytum procumbens extracts and N-acetylglucosamine, we were interested in preparing formulations with these natural substances for topical applications. In the present study, we compared the rheological properties of various creams and gels with bulk and nanoparticle forms of N-acetylglucosamine added, focusing on the flow properties of multiphase emulsion. Moreover, the ability of nanoparticles to reduce inflammation and stimulate collagen production was demonstrated in both chondrocyte and fibroblast spheroids. The results showed the activity of nano-N-acetylglucosamine in our cell models, suggesting its suitability for use as a component in creams and gels. Furthermore, its ability to affect the flow properties of commercial creams and gels makes it an ideal component of topical formulations for the treatment of inflamed skin and joints.

Antimicrobial Preservatives in Cyclodextrin-Containing Drug Formulations.

In general, antimicrobial preservatives are essential components of multidose pharmaceutical formulations to prevent microbial growth and contamination, many of which contain lipophilic and poorly water-soluble drugs in need of solubilizing excipients, such as cyclodextrins (CDs). However, CDs frequently reduce or even abolish the antimicrobial activities of commonly used pharmaceutical preservatives. The degree of inactivation depends on the CD complexation of the preservatives, which in turn depends on their chemical structure and physiochemical properties. In general, lipophilic preservatives are more likely to be inactivated; however, CDs are also known to inactivate highly water-soluble preservatives. In some drug formulations, preservative inactivation has been offset by including excipients that possess some antimicrobial activity on their own. In this review, we explain how CDs interact with some commonly used pharmaceutical preservatives and why some preservatives are more susceptible to CD inactivation than others are.

Formulation, Evaluation and Stability Studies of Dutasteride Loaded Niosomal Gel

Introduction: Dutasteride, a synthetic 4-azasteroid belonging to the class of 5-α-reductase, a BCS class II drug, is used in treating Androgenetic Alopecia and Benign Prostatic Hyperplasia. Aims: The study aims to formulate, evaluate and perform stability studies of Dutasteride-loaded topical niosomal gel. Methodology: Formulation components such as, surfactants and cholesterol were tested for any drug/excipient interactions. Ether injection method was employed to prepare Niosomes. Five formulations were prepared and then assessed for their particle size, SEM, zeta potential, PDI, entrapment efficiency, drug content and in vitro diffusion studies. The optimized formulation F3 Consisted of Dutasteride, span 40 and cholesterol in the ratio 1:4:2. The optimized formulation (F3) was incorporated into a gel. Three gel formulations (FG1, FG2 and FG3) were prepared and were assessed for pH, viscosity, spreadability, drug content and in vitro diffusion studies. The optimized niosomal gel (FG2) consisted of 0.3% Optimized Niosomes and 0.75% Carbopol 934. The drug release kinetics studies were performed for the optimized gel. Finally, stability studies were performed at 30°C ± 2°C / 65% RH ± 5%. Results: The optimized niosomes showed an Entrapment efficiency of 63.2%, zeta potential -22.7 mV, particle size 300.4 nm, drug content 86.23% and 96.23% drug release in 8 hours. The optimized niosomal gel (FG2) consisted of 0.3% Optimized Niosomes and 0.75% Carbopol 934. The gel showed pH 4.7, viscosity 66213 cps, spreadability 15.7g.cm/sec, drug content 91.4% and percent drug release 91.45% in 24 hours. The drug release kinetics studies showed that the optimized gel formulation (FG2) followed Higuchi model with R2 value of 0.9975. The stability studies indicated that the optimized niosomal gel was stable for 90 days. Conclusion: The stability studies confirmed the drug content and the physical nature of the gel for 90 days. Thus, the formulation can be regarded as stable and effective for drugs meant for topical application. Dutasteride gel formulations have the potential to enhance drug bioavailability by facilitating greater penetration of drugs with restricted permeability.

Enhancing 3D-Printed Chocolate Drug Delivery: The Role of Soy Lecithin in Improving Formulation Printability and Consistency

Abstract Objectives This study explores the potential of extrusion-based 3D printing to improve medication adherence by developing chocolate-based oral dosage forms incorporating active pharmaceutical ingredients such as paracetamol and ibuprofen, while using soy lecithin as an emulsifier to enhance the flow properties of the chocolate formulation, enabling consistent and reliable 3D printing of the dosage forms. Methods Extrusion-based 3D printing was used to obtain drug-loaded solid oral dosage forms. The formulation components as well as the printing design and conditions were optimised, to enhance the appearance and patient acceptability of the final products. Techniques such as spectroscopy, thermal analysis, rheology, mechanical analysis and in-vitro dissolution were employed to assess the physicochemical properties of these formulations. Key Findings: Soy lecithin was essential in obtaining robust and consistent dosage forms. The formulations showed good physicochemical stability of the components and demonstrated consistent drug release. Conclusions The findings suggest that extrusion-based 3D printing, with the aid of emulsifiers such as soy lecithin, is a viable method for producing personalised, chocolate-based drug delivery systems, potentially improving adherence through customizable dosage forms. Further research could enhance understanding of factors such as particle size, crystallinity, and the impact of chewing on drug release, to optimise therapeutic outcomes.