Development Of Pharmaceutical Formulations Research Articles

RESPONSE SURFACE METHODOLOGY (RSM) AS A TOOL IN PHARMACEUTICAL FORMULATION DEVELOPMENT

Response surface methodology (RSM) serves as a valuable tool in pharmaceutical formulation development, facilitating the optimization of drug formulations by systematically exploring the effects of multiple variables on desired responses. This methodology involves the design of experiments to generate mathematical models that predict the relationship between formulation parameters and critical quality attributes. By utilizing statistical techniques such as factorial design, central composite design, and Box-Behnken design, RSM enables the identification of optimal formulation conditions while minimizing the number of experimental trials. Across iterative experimentation and model refinement, RSM assists in understanding the complex interactions between formulation components, process variables, and product characteristics. In this review, we discuss the application of RSM in pharmaceutical formulation studies, highlighting its efficacy in optimizing drug delivery systems, enhancing product stability, and ensuring quality control. In addition, we explore recent advancements in RSM-driven approaches, including its integration with computational modeling and artificial intelligence techniques for enhanced formulation design and process optimization. Overall, RSM offers a systematic and efficient approach for developing robust pharmaceutical formulations, thereby accelerating the drug development process and improving therapeutic outcomes.

A Comprehensive Review on Imperative Role of Ionic Liquids in Pharmaceutical Sciences.

Ionic liquids (ILs) are poorly-coordinated ionic salts that can exist as a liquid at room temperatures (or <100 °C). ILs are also referred to as "designer solvents" because so many of them have been created to solve particular synthetic issues. ILs are regarded as "green solvents" because they have several distinctive qualities, including better ionic conduction, recyclability, improved solvation ability, low volatility, and thermal stability. These have been at the forefront of the most innovative fields of science and technology during the past few years. ILs may be employed in new drug formulation development and drug design in the field of pharmacy for various functions such as improvement of solubility, targeted drug delivery, stabilizer, permeability enhancer, or improvement of bioavailability in the development of pharmaceutical or vaccine dosage formulations. Ionic liquids have become a key component in various areas such as synthetic and catalytic chemistry, extraction, analytics, biotechnology, etc., due to their superior abilities along with highly modifiable potential. This study concentrates on the usage of ILs in various pharmaceutical applications enlisting their numerous purposes from the delivery of drugs to pharmaceutical synthesis. To better comprehend cuttingedge technologies in IL-based drug delivery systems, highly focused mechanistic studies regarding the synthesis/preparation of ILs and their biocompatibility along with the ecotoxicological and biological effects need to be studied. The use of IL techniques can address key issues regarding pharmaceutical preparations such as lower solubility and bioavailability which plays a key role in the lack of effectiveness of significant commercially available drugs.

Comparative assessment of physics-based in silico methods to calculate relative solubilities.

Relative solubilities, i.e. whether a given molecule is more soluble in one solvent compared to others, is a critical parameter for pharmaceutical and agricultural formulation development and chemical synthesis, material science, and environmental chemistry. In silico predictions of this crucial variable can help reducing experiments, waste of solvents and synthesis optimization. In this study, we evaluate the performance of different physics-based methods for predicting relative solubilities. Our assessment involves quantum mechanics-based COSMO-RS and molecular dynamics-based free energy methods using OPLS4, the open-source OpenFF Sage, and GAFF force fields, spanning over 200 solvent-solute combinations. Our investigation highlights the important role of compound multimerization, an effect which must be accounted for to obtain accurate relative solubility predictions. The performance landscape of these methods is varied, with significant differences in precision depending on both the method used and the solute considered, thereby offering an improved understanding of the predictive power of physics-based methods in chemical research.

Natural Dyes: A Comprehensive Review on Medicinal Plant-based Pigments and Culinary Herbs as Flavor Enhancers

The global demand for natural dyes has surged, propelled by a growing awareness of the therapeutic properties inherent in these dyes. Derived from a variety of sources such as plants, insects, animals, and minerals, natural dyes have garnered attention as safer alternatives to synthetic colorants, many of which have been banned due to their potential to cause allergy-like symptoms or pose carcinogenic risks. Notably, plant-based pigments among natural dyes exhibit a diverse array of medicinal values. This review provides an in-depth exploration of various types of dyes, highlighting the distinctions between natural and synthetic counterparts and delvloping into their wide-ranging applications. The adverse effects associated with synthetic dyes are discussed, emphasizing the need for sustainable alternatives. The paper also offers a compilation of information on synonyms, biological sources, chemical constituents, and uses found in naturally occurring dye-yielding plants, aiming to contribute to the development of pharmaceutical and cosmeceutical formulations. This comprehensive review amalgamates the realms of natural dyes and culinary herbs, offering valuable insights into their medicinal and culinary significance.

Methodological advances in formulation and assay of herbal resources-based topical drug delivery systems.

Medicinal plants have been utilized for centuries as a source of healing compounds, which consist of thousands of known bioactive molecules with therapeutic potentials. This article aims to explore and emphasize the significance of medicinal plants and bioactive compounds in the development of topical pharmaceutical formulations. The journey from the extraction of phytochemicals to the development of topical pharmaceutical formulations is described with the aid of scientific evidence selected from PubMed, Google Scholar, ScienceDirect, and Web of Science. Articles published in English during 2018-2023 period were considered and selected randomly. The review discusses the extraction process of medicinal plants, solvent selection, and green synthesis of metal nanoparticles. Subsequently, various biological activities of plant extracts are elaborated especially focusing on antimicrobial, antioxidant, anti-inflammatory, and sun protection activities, along with the corresponding invitro assays commonly employed for the evaluation. The article presents the process of compound isolation through bioactivity-guided fractionation and also the toxicity evaluation of isolated fractions. Finally, the formulation of medicinal plant extracts into topical pharmaceuticals is addressed, emphasizing the stability evaluation procedures necessary for ensuring product quality and efficacy.

Hemocompatibility and hemorheological activity of aqueous extracts from Phyllanthus sellowianus: effects on in vitro glycated erythrocytes

IntroductionPhyllanthus sellowianus (Klotzsch) Müll Arg. is an Argentinian and Brazilian native plant used to treat diabetes. In vascular diseases like diabetes, erythrocytes form anomalous aggregates resistant to dissociation, associated with high glucose levels. This work aims to evaluate the hemocompatibility and hemorheological activity of aqueous extracts from P. sellowianus and its anti-diabetic activity using in vitro glycated erythrocytes as occur by hyperglycemia. MethodsFor this work, P. sellowianus specimens were collected on the Nogoyá River coast, Argentina, and morphoanatomical identified. Infusion, maceration, digestion, and cooking extracts were prepared with collected leaves and bark using saline as solvent. The osmolality and pH of the extracts were adjusted to an adequate interaction with human cells. Red blood cells (RBCs) from healthy donors (n=3) were used and incubated with glucose solution for in vitro simulation of the hyperglycemia effects. RBCs were incubated with the aqueous extracts to assess their hemocompatibility. Also, glycated RBCs were incubated with the extracts to analyze their anti-diabetic properties. Erythrocyte Rheometer and Optical Chip Aggregameter were used for the hemorheological evaluation. ResultsAssays with the different P. sellowianus extracts modified the viscoelasticity and aggregation of RBCs. Moreover, in some cases, P. sellowianus extracts reversed the in vitro glycation effect and hemorheological parameters got nearer control values. ConclusionThese results would be helpful for the development of pharmaceutical formulations using this species or its phytocomponents. They also give relevant information to understand the action mechanisms through which these extracts or their components can be used as anti-diabetics in Phytomedicine.

Recent Developments and Applications of 3D-Printing Technology in Pharmaceutical Drug Delivery Systems: A New Research Direction and Future Trends.

The advent of 3D printing technology has emerged as a key technical revolution in recent years, enabling the development and production of innovative medication delivery methods in the pharmaceutical sector. The designs, concepts, techniques, key challenges, and potential benefits during 3D-printing technology are the key points discussed in this review. This technology primarily enables rapid, safe, and low-cost development of pharmaceutical formulations during the conventional and additive manufacturing processes. This phenomenon has wide-ranging implications in current as well as future medicinal developments. Advanced technologies such as Ink-Jet printing, drop-on-demand printing, Zip dose, Electrohydrodynamic Printing (Ejet) etc., are the current focus of the drug delivery systems for enhancing patient convenience and improving medication compliance. The current and future applications of various software, such as CAD software, and regulatory aspects in 3D and 4D printing technology are discussed briefly in this article. With respect to the prospective trajectory of 3D and 4D printing, it is probable that the newly developed methods will be predominantly utilized in pharmacies and hospitals to accommodate the unique requirements of individuals or niche groups. As a result, it is imperative that these technologies continue to advance and be improved in comparison to 2D printing in order to surmount the aforementioned regulatory and technical obstacles, render them applicable to a vast array of drug delivery systems, and increase their acceptability among patients of every generation.

Novel therapeutic deep eutectic system for the enhancement of ketoconazole antifungal activity and transdermal permeability

In this study, we reported the investigation of a novel therapeutic deep eutectic system (THEDES) formed between capric acid (CA) and ketoconazole (KCZ) to enhance the permeability and efficacy of the antifungal drug KCZ. A THEDES was formulated by combining KCZ and CA at different molar ratios, with a 1:5 ratio (K5) representing the most stable and lowest melting point. Characterization of the interactions between CA and KCZ using NMR and FT-IR spectroscopy revealed a hydrogen bonding interaction between the amine group of KCZ’s imidazole ring and the carboxylic acid moiety of CA. This interaction resulted in converting the solid materials into liquid at room temperature, leading to a significant decrease in the melting points of the components, as confirmed by DSC. Next, the effectiveness of K5 as an antifungal agent against Candida albicans was evaluated. The results indicated a 2-fold reduction in the minimum inhibitory concentration (MIC). In addition, permeability studies conducted using a Franz diffusion cell revealed a significant enhancement in permeability with a 6.19-fold increase in flux compared to commercially available KCZ cream. The findings suggest that fatty acid-based deep eutectic systems, such as the KCZ THEDES, can serve as effective and green drug delivery systems, offering significant enhancements in drug permeability and therapeutic performance. This approach improves the efficacy of drugs and promotes the development of eco-friendly pharmaceutical formulations.

Enhancing Dissolution and Bioavailability: A Review on Co-Processed Superdisintegrants in Pharmaceutical Formulations

Co-processed superdisintegrants have emerged as key excipients in pharmaceutical formulation development, offering solutions to challenges related to poor solubility, bioavailability, and patient compliance. This comprehensive review article provides an in-depth analysis of the principles, mechanisms, manufacturing techniques, and applications of co-processed superdisintegrants in drug delivery systems. The review highlights the role of co-processed excipients in enhancing dissolution kinetics, improving formulation efficiency, and enabling innovative drug delivery platforms such as personalized medicine and combination therapies. Regulatory considerations, quality standards, and future directions for research and innovation in this field are also discussed. Through a synthesis of current literature and insights into emerging trends, this review aims to provide researchers, formulation scientists, and pharmaceutical professionals with a comprehensive understanding of the potential and challenges associated with co-processed superdisintegrants in pharmaceutical formulations. Ultimately, the integration of co-processed excipients into formulation development holds promise for advancing drug delivery technology, improving therapeutic outcomes, and addressing unmet medical needs in patient care. Keywords: Co-processed superdisintegrants, Dissolution enhancement, Bioavailability, Pharmaceutical formulations, Drug delivery systems, Excipients, Formulation optimization, Manufacturing techniques, Regulatory considerations, Future directions

From Powder to Structure: Multi-Dimensional Electron Diffraction to Enhance Small Molecule Pharmaceutical Formulation Characterization and Development

From Powder to Structure: Multi-Dimensional Electron Diffraction to Enhance Small Molecule Pharmaceutical Formulation Characterization and Development

Current Updated Review on Applications of Different Grades of Sylysia in Pharmaceutical Formulation Development

Current Updated Review on Applications of Different Grades of Sylysia in Pharmaceutical Formulation Development

Insight into the Manipulation Mechanism of Polymorphic Transformation by Polymers: A Case of Cimetidine.

Employing polymer additives is an effective strategy to realize the manipulation of polymorphic transformation. However, the manipulation mechanism is still not clear, which limit the precise selection of polymeric excipients and the development of pharmaceutical formulations. The solubility of cimetidine (CIM) in acetonitrile/water mixtures were measured. And the polymorphic transformation from CIM form A to form B with the addition of different polymers was monitored by Raman spectroscopy. Furthermore, the manipulation effect of polymers was determined based on the results of experiments and molecular simulations. The solubility of form A is consistently higher than that of form B, which indicate that form B is the thermodynamically stable form within the examined temperature range. The presence of polyvinylpyrrolidone (PVP) of a shorter chain length could have a stronger inhibitory effect on the phase transformation process of metastable form, whereas polyethylene glycol (PEG) had almost no impact. The nucleation kinetics experiments and molecular dynamic simulation results showed that only PVP molecules could significantly decrease the nucleation rate of CIM, due to the ability of reducing solute molecular diffusion and solute-solute molecular interaction. A combination of crystal growth rate measurements and calculations of the interaction energies between PVP and the crystal faces of CIM indicate that smaller molecular weight PVP can suppress crystal growth more effectively. PVP K16-18 has more impact on the stabilization of CIM form A and inhibition of the phase transformation process. The manipulation mechanism of polymer additives in the polymorphic transformation of CIM was proposed.

Green synthesis of silver nanoparticles using food supplement from Avena sativa L., and their antioxidant, antiglycation, and anti-aging activities: In vitro and in silico studies

Food supplement of Avena sativa L. dry extract (AsDE) is produced with green leaves of wild oats and it is commonly used in patients with cognitive disorders and muscle deficits. These symptoms and pathologies can be promoted and/or aggravated by oxidative stress and protein glycation. In order to prevent or treat these disorders, new formulations that could enhance and benefit AsDE have been developed and the formation of metallic nanoparticles by green synthesis has shown to be an alternative. Thus, this study aimed to prepare silver nanoparticles (AgNPs) by green synthesis using AsDE and characterize these AgNPs. Besides, it aimed to evaluate in vitro antioxidant and antiglycation activities of AsDE and AgNPS, and analyze in vitro and in silico inhibitory action on aging enzymes (collagenase, elastase, and tyrosinase). UV–visible spectroscopy, Zeta potential and scanning transmission electron microscopy were used to characterize AgNPs. Antioxidant activity was determined by DPPH free radical scavenging, ferric ion reducing power (FRAP), lipid peroxidation inhibition, ABTS radical scavenging, and oxygen radical absorption capacity (ORAC). Molecular docking analyses were performed to evaluate interactions between the major compounds of AsDE and aging enzymes or DNA. Antioxidant tests demonstrated antioxidant activity of 19.67 % for AsDE and 42.98 % for AgNPs in DPPH test; and 115.67 µM Trolox Equivalent (TE)/g for AsDE and 554.33 µM TE/g for AgNPs in FRAP test. In addition, AsDE and AgNPs inhibited 25.40 % and 11.33 % of lipid peroxidation, respectively, and presented 255.22 µM TE/g for AsDE and 317.44 µM TE/g for AgNPs in ABTS test. AsDE and AgNPs exhibited antioxidant potential observed in ORAC assay. In addition, AsDE presented inhibitory action on collagenase, elastase and tyrosinase activities (78.23 %, 68.14 % and 62.27 % inhibition, respectively). Antiglycation tests demonstrated that bovine serum albumin exposed to ribose and treated with AsDE at 0.5 mg/mL exhibited the highest percentage of free amino groups (45.21 %), while samples treated with AgNPs showed 35.41 % free amino groups. On the other hand, AgNPs exhibited the highest percentage of inhibition of advanced glycation end-products formation (85.75 %), which did not differ from aminoguanidine, a known antiglycation agent. Besides, relative electrophoretic mobility assay demonstrated that samples treated with AsDE at 0.1 mg/mL or AgNPs showed antiglycation activity comparable to aminoguanidine. The in silico assays showed interactions between the major compounds of AsDE and aging enzymes or DNA. Therefore, results represent an important indicator for the development and discovery of new nanostructured pharmaceutical and cosmetic formulations using plants and their bioactive compounds.

HPLC-UV method for the quantification of a novel indole-thiazole derivative (CS08) in nanoparticles

BackgroundValidation of an analytical method for the quantification of a drug candidate molecule is the first step. The quantification method is fundamental in the pharmaceutical industry, as it allows the development of a pharmaceutical product, such as encapsulation in nanocarriers. ObjectiveTo validate the quantification method of a novel indole-thiazole derivative (CS08) by HPLC-UV in nanoparticles. MethodsWe developed a quantification method using an HPLC coupled to a UV detector, and evaluated the method for its selectivity, linearity, precision, accuracy, LOD, LOQ, and robustness. With the method, we evaluated the stability of CS08 in different pHs simulating biological media and quantified the encapsulation rate in dextran- or fucoidan-coated nanoparticles. ResultsIt was possible to quantify CS08 using the method in different matrices, proving to be a selective, linear, precise, accurate, and robust method in the determined concentrations (1–20 µg.mL−1). The LOD and LOQ were low on a microgram scale, which facilitates the quantification of CS08 for the development of pharmaceutical formulations, showing confidence in the results obtained from the rate of encapsulation in nanoparticles. ConclusionThe validated method proved to be adequate for the quantification of CS08 in different matrices, allowing the evaluation of its encapsulation rate in nanoparticles.

A Novel image processing technique for weighted particle size distribution assessment

The objective of the study was to create a reliable method that could be used to evaluate the particle size distribution of samples and pre-mixes in real-world situations, particularly those consisting of typical formulation blends. The goal was to use this method to assess the uniformity of the samples and ensure that they met the required quality standards. The researchers aimed to create a method that could be easily incorporated into the manufacturing process, providing a practical and efficient solution. This study demonstrates the use of ImageJ software to analyze the particle size distribution (PSD) of powders. The technique produces qualitative data from microscopy images and quantitative data from analysis of parameters including average diameter, D 10, D 50 , D 90, and standard deviation. The method was tested with various treatments, showing differentiating outcomes in all cases. The alternate technique provides a rapid and cost-effective method for PSD analysis, surpassing the limitations of sieve analysis. Extensive testing of the method, using a variety of sample types, including typical formulation blends, was performed. The results suggest that the method can effectively assess the morphology of changing materials during batch manufacturing and characterize uniformity in blends. The methodology has the capability to identify attributes related to PSD that are typically required to be monitored during manufacturing. The technique allows for accurate and reliable quantification of the attributes through image capture technology. The technique has future potential and has important implications for material science, powder rheology, pharmaceutical formulation development, and continual process monitoring.

Health is the greatest wealth: Quest for a diagnostic check for thermochemistry of pure drug compounds

The development of pharmaceutical formulations and the optimisation of drug synthesis are not possible without knowledge of thermodynamics. At the same time, the quantity and quality of the available data is not at a level that meets modern requirements. A convenient diagnostic approach is desirable to assess the quality of available experimental thermodynamic data of drugs. A comprehensive set of available data on phase transitions of profens family drugs was analysed using new complementary measurements and structure–property correlations. The consistent sets of solid–gas, liquid–gas and solid–liquid phase transitions were evaluated for twelve active pharmaceutical ingredients based on alkanoic acid derivatives and recommended for the calculations of the pharmaceutical processes. A “centerpiece approach” proposed in this work helped to perform the “health check” of the thermochemical data. The evaluated data on the sublimation enthalpies were used to derive the crystal lattice energies of the profens and to correlate the water solubilities with the sublimation vapour pressures and molecular parameters. A “paper-and-pen” approach proposed in this work can be extended to the diagnosis of “sick” or “healthy” thermodynamic data for drugs with a different structure than those studied in this work.

New RP-HPLC method for the simultaneous determination of process yield and percentage of encapsulation of Gallein in albumin nanoparticles

A study was performed for the development and validation of a method of High Performance Liquid Chromatography (HPLC) for the identification and simultaneous quantification of Gallein and Human Serum Albumin (HSA). In addition, this work presents the development and physicochemical characterization of this new pharmaceutical formulation of HSA nanoparticles loaded with Gallein for potential use in the treatment of Alzheimer’s disease.The method was developed with the purpose of determining the performance of the synthesis process of nanoparticles and the efficiency of encapsulation of the drug in the nanosystem. The HPLC mobile phase consisted of ACN:H2O:TEA:H3PO4 (50:49.8:0.1:0.1 v/v/v) pumped at a flow rate of 0.8 mL/min, isocratic mode, and the measurement were carried out at 220 nm. Chromatographic runs were performed on a C18 column (150 × 4.60 mm; 5 μm size particles). The HPLC-method was validated following the International Conference on Harmonisation (ICH) of Technical Requirements for Registration of Pharmaceuticals for Human Use guidelines and was used to simultaneously quantify the two components of the nanoformulation. Thus, the values obtained through the validated method were 43 % for drug encapsulation efficiency (% EE) and the synthesis performance (% yield) was 96 %.Moreover, the nanoformulation was characterized by DLS, the results showed that the average particle size was 217 nm, with a PDI of (0.085 ± 0.005) and a potential Z of −29.7 mV.Therefore, the developed method has proven useful in providing accurate simultaneous measurements of HSA and Gallein from albumin nanoparticles. It is advantageous since it is able to reduce the time and facilitate the determination of Gallein encapsulation efficiency and yield of albumin nanoparticles.

From Scraps to Solutions: Harnessing the Potential of Vegetable and Fruit Waste in Pharmaceutical Formulations

Background:: Food waste is a major worldwide problem due to the increasing population and imbalances in supply chains. Waste from fruits and vegetables are a substantial proportion of the overall food waste generated, accounting for approximately 42% of the waste produced. Methane, a strong greenhouse gas with a significant potential for global warming, is produced when these waste products are typically dumped in landfills. Objectives:: The study's goal is to present a thorough overview of the most recent findings and developments in the use of vegetable and fruit waste for creating therapeutic formulations. Recognizing the opportunities and challenges in this developing area of study, as well as the promise that vegetable and fruit waste contains for the creation of environmentally friendly and economically advantageous pharmaceutical formulations. Methods:: A comprehensive review of existing literature on the utilization of vegetable and fruit waste in pharmaceutical formulations was conducted. The review included studies on the chemical composition and bioactive compounds present in various types of vegetable and fruit waste, their extraction methods, and their potential applications in pharmaceutical formulations. Additionally, current waste management practices and challenges associated with waste disposal were also analyzed. Conclusion:: The review highlights the significant potential of vegetable and fruit waste in the development of pharmaceutical formulations. Fruit and vegetable waste offer a wide range of bioactive compounds, such as antioxidants, antimicrobials, and antiinflammatory agents, which could be utilized in drug formulation. Moreover, this approach can promote environmental sustainability by reducing waste generation and enhancing waste utilization. Further research and development efforts should focus on optimizing extraction methods, evaluating the efficacy and safety of wastederived compounds, and addressing regulatory requirements for integrating vegetable and fruit waste into pharmaceutical products. Harnessing the potential of vegetable and fruit waste in pharmaceutical formulations can lead to sustainable advancements in the pharmaceutical industry while addressing environmental concerns.

Almond fixed oil from Syagrus coronata (Mart.) Becc. has antinociceptive and anti-inflammatory potential, without showing oral toxicity in mice

Ethnopharmacological relevanceSyagrus coronata, a palm tree found in northeastern Brazil, popularly known as licuri, has socioeconomic importance for the production of vegetable oil rich in fatty acids with nutritional and pharmacological effects. Licuri oil is used in traditional medicine to treat inflammation, wound healing, mycosis, back discomfort, eye irritation, and other conditions. Aim of the studyThe study aimed to evaluate the antinociceptive, anti-inflammatory, and antipyretic effects of treatment with Syagrus coronata fixed oil (ScFO), as well as to determine the safety of use in mice. Materials and methodsInitially, the chemical characterization was performed by gas chromatography-mass spectrometry. Acute single-dose oral toxicity was evaluated in mice at a dose of 2000 mg/kg. Antinociceptive activity was evaluated through abdominal writhing, formalin, and tail dipping tests, and the anti-inflammatory potential was evaluated through the model of acute inflammation of ear edema, peritonitis, and fever at concentrations of 25, 50, and 100 mg/kg from ScFO. ResultsIn the chemical analysis of ScFO, lauric (43.64%), caprylic (11.7%), and capric (7.2%) acids were detected as major. No mortality or behavioral abnormalities in the mice were evidenced over the 14 days of observation in the acute toxicity test. ScFO treatment decreased abdominal writhing by 27.07, 28.23, and 51.78% at 25, 50, and 100 mg/kg. ScFO demonstrated central and peripheral action in the formalin test, possibly via opioidergic and muscarinic systems. In the tail dipping test, ScFO showed action from the first hour after treatment at all concentrations. ScFO (100 mg/kg) reduced ear edema by 63.76% and leukocyte and neutrophil migration and IL-1β and TNF-α production in the peritonitis test. ConclusionMice treated with ScFO had a reduction in fever after 60 min at all concentrations regardless of dose. Therefore, the fixed oil of S. coronata has the potential for the development of new pharmaceutical formulations for the treatment of pain, inflammation, and fever.

Optimizing Process Parameters for Controlled Drug Delivery: A Quality by Design (QbD) Approach in Naltrexone Microspheres.

The formulation of microspheres involves a complex manufacturing process with multiple steps. Identifying the appropriate process parameters to achieve the desired quality attributes poses a significant challenge. This study aims to optimize the critical process parameters (CPPs) involved in the preparation of naltrexone microspheres using a Quality by Design (QbD) methodology. Additionally, the research aims to assess the drug release profiles of these microspheres under both in vivo and in vitro conditions. Critical process parameters (CPPs) and critical quality attributes (CQAs) were identified, and a Box-Behnken design was utilized to delineate the design space, ensuring alignment with the desired Quality Target Product Profile (QTPP). The investigated CPPs comprised polymer concentration, aqueous phase ratio to organic phase ratio, and quench volume. The microspheres were fabricated using the oil-in-water emulsion solvent extraction technique. Analysis revealed that increased polymer concentration was correlated with decreased particle size, reduced quench volume resulted in decreased burst release, and a heightened aqueous phase ratio to organic phase ratio improved drug entrapment. Upon analyzing the results, an optimal formulation was determined. In conclusion, the study conducted in vivo drug release testing on both the commercially available innovator product and the optimized test product utilizing an animal model. The integration of in vitro dissolution data with in vivo assessments presents a holistic understanding of drug release dynamics. The QbD approach-based optimization of CPPs furnishes informed guidance for the development of generic pharmaceutical formulations.