Drug Release Kinetics Research Articles

Innovative Vesicular Drug Delivery Systems: Unleashing the Power of Nanocarriers

"Drug delivery systems utilizing vesicular nanocarriers represent a revolutionary approach in modern pharmaceutical science. These innovative systems harness the potential of nanotechnology to enhance therapeutic efficacy, improve drug bioavailability, and mitigate adverse effects. Vesicular nanocarriers, encompassing liposomes, niosomes, ethosomes, and transfersomes among others, exhibit remarkable versatility in encapsulating diverse pharmaceutical agents, ranging from small molecules to biologics. Their unique structural properties and tunable characteristics enable precise modulation of drug release kinetics, facilitating targeted delivery and controlled release at the desired site of action. Moreover, these nanocarriers offer inherent advantages, including increased stability, reduced toxicity, and the potential to overcome biological barriers, thereby revolutionizing the landscape of drug delivery. This abstract explores the state-of-the-art advancements, promising applications, and future prospects of vesicular nanocarriers, shedding light on their transformative role in optimizing therapeutic outcomes and paving the way for personalized medicine."

Exploring Cyclodextrin-Based Nanosponges as Drug Delivery Systems: Understanding the Physicochemical Factors Influencing Drug Loading and Release Kinetics.

Cyclodextrin-based nanosponges (CDNSs) are complex macromolecular structures composed of individual cyclodextrins (CDs) and nanochannels created between cross-linked CD units and cross-linkers. Due to their unique structural and physicochemical properties, CDNSs can possess even more beneficial pharmaceutical features than single CDs. In this comprehensive review, various aspects related to CDNSs are summarized. Particular attention was paid to overviewing structural properties, methods of synthesis, and physicochemical analysis of CDNSs using various analytical methods, such as DLS, PXRD, TGA, DSC, FT-IR, NMR, and phase solubility studies. Also, due to the significant role of CDNSs in pharmaceutical research and industry, aspects such as drug loading, drug release studies, and kinetics profile evaluation of drug-CDNS complexes were carefully reviewed. The aim of this paper is to find the relationships between the physicochemical features and to identify crucial characteristics that are influential for using CDNSs as convenient drug delivery systems.

Lipid-Polymer Hybrid Nanoparticles Synthesized via Lipid-Based Surface Engineering for a robust drug delivery platform

Herein, lipid-polymer core-shell hybrid nanoparticles composed of poly(D,L-lactic-co-glycolic acid) (PLGA)/lecithin (PLNs) were synthesized through lipid-based surface engineering. Lipids were absorbed onto the surface of the PLGA core to enhance the advantages of polymeric nanoparticles and liposomes. The amounts of lipids and encapsulation of the drug nicardipine hydrochloride (NCH) in the PLNs were studied. NCH-loaded PLNs (NCH-PLNs) were produced in high yield (66%) with a high encapsulation efficiency (92%) and a size of 176 nm. The mass of phosphorus (P) on the NCH-PLN surface was qualitatively and quantitatively investigated using X-ray fluorescence spectroscopy, and lecithin addition increased the P mass percentage due to the phosphate group (PO43-) in its structure. These data confirmed the lipid-based surface engineering of NCH-PLNs. The zeta potential of NCH-PLN exceeded −30 mV, ensuring colloidal stability, and preventing precipitation through electrostatic stabilization. In vitro, NCH was continuously and slowly released from NCH-PLNs over 16 days. Furthermore, PSVK1 cells exhibited high viability after treatment with NCH-PLNs, indicating favorable cytocompatibility. After comparing various mathematical equations of drug release kinetics, the data best fit the Korsmeyer-Peppas model with R2 values of 0.989, 0.990, and 0.982 for 1.0, 3.0, and 5.0 mg/mL lecithin, respectively. The release exponents obtained ranged from 0.480 to 0.505, suggesting anomalous transport release. Thus, NCH-PLNs have potential as a robust drug delivery platform for the controlled administration of NCH, particularly for vasodilation during neurosurgery.

Advancing Breast Cancer Drug Delivery: The Transformative Potential of Bioinformatics and Artificial Intelligence

Abstract: Breast cancer remains a significant global health challenge, necessitating innovative approaches to improve treatment efficacy while minimizing side effects. This review explores the promising advancements in breast cancer drug delivery driven by the transformative potential of bioinformatics and Artificial Intelligence (AI). Bioinformatics plays a pivotal role in unraveling the intricate genomic landscape of breast cancer, enabling the identification of potential drug targets and biomarkers. The integration of multi-omics data facilitates a comprehensive understanding of the disease, guiding personalized treatment strategies. Moreover, bioinformatics-driven approaches aid in biomarker discovery and prediction, offering novel tools for prognosis and treatment response assessment. AI, particularly machine learning and deep learning, has revolutionized breast cancer research. Machine learning models empower accurate diagnosis through image analysis, improve survival prediction, and enhance risk assessment. Deep learning algorithms, such as convolutional neural networks, enable precise tumor detection and classification from medical imaging data, notably mammograms and MRI scans. Additionally, natural language processing techniques facilitate the mining of vast scientific literature, uncovering hidden insights and identifying potential drug targets. Network-based approaches integrated with AI algorithms facilitate the identification of central proteins as promising drug targets within complex biological networks. This review also examines AIoptimized nanoformulations designed to enhance targeted drug delivery. AI-guided design of drugloaded nanoparticles improves drug encapsulation efficiency, release kinetics, and site-specific delivery, offering promising solutions to overcome the challenges of conventional drug delivery.

Biodegradable Local Chemotherapy Platform with Prolonged and Controlled Release of Doxorubicin for the Prevention of Local Tumor Recurrence.

Local recurrence after surgical and therapeutic treatment remains a significant clinical problem in oncology. Recurrence may be due to imperfections in existing therapies, particularly chemotherapy. To improve antitumor activity and prevent local cancer recurrence while keeping toxicity at acceptable levels, we have developed and demonstrated a biodegradable local chemotherapy platform that provides controlled and prolonged drug release. The platform consists of a polycaprolactone (PCL) substrate, which provides the structural integrity of the platform and the predominant unidirectional drug release, and a thin multilayer coating (∼200 nm) containing doxorubicin (DOX). The coating is an electrostatic complex obtained by the layer-by-layer (LbL) assembly and consists of natural polyelectrolytes [poly-γ-glutamic acid (γ-PGA) and chitosan (CS) or poly-l-lysine (PLL)]. To improve the release stability, an ionic conjugate of DOX and γ-PGA was prepared and incorporated into the multilayer coating. By varying the structure of the coating by adding empty (without DOX) bilayers, we were able to control the kinetics of drug release. The resulting platforms contained equal numbers of empty bilayers and DOX-loaded bilayers (15 + 15 or 30 + 30 bilayers) with a maximum loading of 566 ng/cm2. The platforms demonstrated prolonged and fairly uniform drug release for more than 5 months while retaining antitumor activity in vitro on ovarian cancer cells (SKOV-3). The empty platforms (without DOX) showed good cytocompatibility and no cytotoxicity to human fibroblasts and SKOV-3 cells. This study presents the development of a local chemotherapy platform consisting of a PCL-based substrate which provides structural stability and a biodegradable polyelectrolyte layered coating which combines layers containing a polyanion ionic complex with DOX with empty bilayers to ensure prolonged and controlled drug release. Our results may provide a basis for improving the efficacy of chemotherapy using drug delivery systems.

Green LC-MS/MS method for in-vivo pharmacokinetics of mirabegron-encapsulated nanostructured lipid carriers in rat plasma: Integrating white analytical chemistry and analytical quality by design approach

Mirabegron (MBG) stands as the top choice for managing overactive bladder, yet its limited aqueous solubility and low bioavailability pose significant challenges. To overcome these hurdles, the objective was to develop and characterize nanostructured lipid carriers (NLCs) for mirabegron, facilitating its controlled release for overactive bladder treatment through the Quality by Design (QbD) approach. The literature showcases several analytical techniques for mirabegron quantification in pharmaceutical formulations and biological fluids, yet most employ toxic organic solvents in their mobile phases, posing environmental risks and threats to aquatic life. To address this concern, a green liquid chromatographic-tandem mass spectrometry method was developed for in-vivo pharmacokinetic assessment of mirabegron-loaded NLCs in rat plasma, utilizing safe organic solvents. The method's development embraced the principles of analytical QbD, aiming to curtail organic waste generation during sample analysis. Rigorous validation was conducted in accordance with the International Council for Harmonization (ICH) Q2 (R1) and M10 guidelines. The developed method found application in both in-vitro drug release kinetics and in-vivo pharmacokinetic investigations of mirabegron-loaded NLCs. Its performance was assessed using the principles of green and white analytical chemistry through a comparative study with existing analytical techniques. The proposed method's exceptional sensitivity, robustness, and eco-friendliness in mirabegron estimation were highlighted by the results. In conclusion, this proposed green analytical approach not only provides a reliable means of mirabegron analysis but also aligns with sustainable practices by minimizing environmental impact and promoting the principles of green and white analytical chemistry and analytical quality by design.

Spray-Dried Chitosan Hydrogel Particles as a Potential Delivery System for Benzydamine Hydrochloride.

Chitosan, being a biocompatible and mucoadhesive polysaccharide, is one of the most preferred hydrogel-forming materials for drug delivery. The objectives of the present study are to obtain spray-dried microparticles based on low-molecular-weight chitosan and study their potential application as cargo systems for the orally active drug benzydamine hydrochloride. Three types of particles are obtained: raw chitosan particles (at three different concentrations), cross-linked with sodium tripolyphosphate (NaTPP) particles (at three different chitosan:NaTPP ratios), and particles coated with mannitol (at three different chitosan:mannitol ratios), all of them in the size range between 1 and 10 µm. Based on the loading efficiency and the yields of the formulated hydrogel particles, one model of each type is chosen for further investigation of the effect of the cross-linker or the excipient on the properties of the gel structures. The morphology of both empty and benzydamine hydrochloride-loaded chitosan particles was examined by scanning electron microscopy, and it was quite regular and spherical. Interactions and composition in the samples are investigated by Fourier-transformed infrared spectroscopy. The thermal stability and phase state of the drug and drug-containing polymer matrixes were tested by differential scanning calorimetry and X-ray powdered diffraction, revealing that the drug underwent a phase transition. A drug release kinetics study of the chosen gel-based structures in simulated saliva buffer (pH = 6.8) and mathematical modeling of the process were performed, indicating the Weibull model as the most appropriate one.

Envisioning the Future: Nanomicelles Revolutionizing Ocular Drug Delivery.

Due to the complexities of the eye's anatomy and physiology, achieving targeted drug delivery with minimal harm to healthy eye tissues has proven to be difficult. The focus of the review is on the potential of lipid and polymer micelle-based drug delivery systems, specifically nanomicelles, to overcome these challenges and improve the absorption of insoluble drugs. Nanomicelles offer several advantages, such as enhanced drug release kinetics, increased drug incorporation, and improved formulation of hydrophobic medicines. The review provides insights into various excipients, preparation methods, and evaluation techniques used in nanomicellar-based drug delivery systems. Furthermore, the review highlights current research and patents related to nanomicelles in ocular drug delivery, suggesting growing interest and potential for future developments in this field. Nanomicelles present a promising approach that may revolutionize ocular drug delivery and open new possibilities for treating various ocular diseases while minimizing adverse effects on healthy eye tissues.

Insights into Targeted and Stimulus-Responsive Nanocarriers for Brain Cancer Treatment.

Brain cancers, especially glioblastoma multiforme, are associated with poor prognosis due to the limited efficacy of current therapies. Nanomedicine has emerged as a versatile technology to treat various diseases, including cancers, and has played an indispensable role in combatting the COVID-19 pandemic as evidenced by the role that lipid nanocarrier-based vaccines have played. The tunability of nanocarrier physicochemical properties -including size, shape, surface chemistry, and drug release kinetics- has resulted in the development of a wide range of nanocarriers for brain cancer treatment. These nanocarriers can improve the pharmacokinetics of drugs, increase blood-brain barrier transfer efficiency, and specifically target brain cancer cells. These unique features would potentially allow for more efficient treatment of brain cancer with fewer side effects and better therapeutic outcomes. This review provides an overview of brain cancers, current therapeutic options, and challenges to efficient brain cancer treatment. The latest advances in nanomedicine strategies are investigated with an emphasis on targeted and stimulus-responsive nanocarriers and their potential for clinical translation.

Co-assembly of Amphiphilic Triblock Copolymers with Nanodrugs and Drug Release Kinetics in Solution.

Polymeric vesicles present great potential in disease treatment as they can be featured as a structurally stable and easily functionalized drug carrier that can simultaneously encapsulate multiple drugs and release them on-demand. Based on the dissipative particle dynamics (DPD) simulation, the drug-loaded vesicles were designed by the co-assembly process of linear amphiphilic triblock copolymers and hydrophobic nanodrugs in solvents, and most importantly, the drug release behavior of drug-loaded vesicles were intensively investigated. The drug-loaded aggregates, such as vesicles, spherical micelles, and disk-like micelles, were observed by varying the size and concentration of nanodrugs and the length of the hydrophobic block. The distribution of nanodrugs in the vesicles was intensively analyzed. As the size of the nanodrugs increases, the localization of nanodrugs change from being unable to fully wrap in the vesicle wall to the uniform distribution and finally to the aggregation in the vesicles at the fixed concentration of nanodrugs. The membrane thickness of the drug-loaded polymeric vesicle can be increased, and the nanodrugs localized closer to the center of the vesicle by increasing the length of the hydrophobic block. The nanodrugs will be released from vesicles by varying the interactions between the nanodrug and the solvent or the hydrophobic block and the solvent, respectively. We found that the release kinetics conforms to the first-order kinetic model, which can be used to fit the cumulative release rate of nanodrugs over time. The results showed that increasing the size of nanodrugs, the length of hydrophobic block, and the interaction parameters between the hydrophobic block and the solvent will slow down the release rate of the nanodrug and change the drug release process from monophasic to biphasic release model.

Dexamethasone nanomedicines with optimized drug release kinetics tailored for treatment of site-specific rheumatic musculoskeletal diseases

The application of polymer-based drug delivery systems is advantageous for improved pharmacokinetics, controlled drug release, and decreased side effects of therapeutics for inflammatory disease. Herein, we describe the synthesis and characterization of linear N-(2-hydroxypropyl)methacrylamide-based polymer conjugates designed for controlled release of the anti-inflammatory drug dexamethasone through pH-sensitive bonds. The tailored release rates were achieved by modifying DEX with four oxo-acids introducing reactive oxo groups to the DEX derivatives. Refinement of reaction conditions yielded four well-defined polymer conjugates with varied release profiles which were more pronounced at the lower pH in cell lysosomes. In vitro evaluations in murine peritoneal macrophages, human synovial fibroblasts, and human peripheral blood mononuclear cells demonstrated that neither drug derivatization nor polymer conjugation affected cytotoxicity or anti-inflammatory properties. Subsequent in vivo tests using a murine arthritis model validated the superior anti-inflammatory efficacy of the prepared DEX-bearing conjugates with lower release rates. These nanomedicines showed much higher therapeutic activity compared to the faster release systems or DEX itself.

PREPARATION AND JUSTIFICATION OF NANOFIBRES-LOADED MAFENIDE USING ELECTROSPINNING TECHNIQUE TO CONTROL RELEASE

Objective: The primary objective was to fabricate a novel drug delivery system capable of providing a controlled and prolonged release of antibiotics. Methods: The experimental design was formulated using Design-Expert® software (version 13), enabling systematic and efficient fabrication process optimization. The study involved the preparation of various nanofiber formulations with different ratios of the three polymers to assess their impact on drug release behavior. Mafenide, a widely used antibiotic, was chosen as the model drug for this investigation. The electrospinning process allowed for producing uniform and fine nanofibers with a high surface area, ensuring a large drug-loading capacity. The synthesized nanofibers were characterized using scanning electron microscopy (SEM) and Fourier transform infrared spectroscopy (FTIR) to evaluate their morphology, chemical interactions, and thermal properties. The drug release kinetics of the antibiotic-loaded nanofibers were studied under different physiological conditions to assess their sustained release behavior. Results: The final nanofiber formula was successfully prepared using the electrospinning technique. The Fourier Transform Infrared Spectroscopy (FTIR) analysis was achieved to confirm the possibility of chemical interaction and bond formation between mafenide and the polymers. Present. The SEM picture of the optimized nanofiber formula showed the homogeneity and excellent entanglement of the electrospun nanofibers at a resolution of 5 µm. PVA/chitosan/HPMC and mafenide pure drug have been successfully fabricated with sufficient strength to resist swelling after absorbing wound exudate. The polymer network becomes more compact when chitosan and Hydroxypropyl Methyl Cellulose (HPMC) are combined with polyvinyl alcohol (PVA), enabling regulated swelling during solvent ingress. The polymer composite's three-dimensional network influenced how quickly the medication was released from the matrix. Sample 2's polymer network traps the medication, gradually releasing after controlled swelling, resulting in a sustained release profile compared to blank sample according to the cumulative release (%) study of mafenide loaded nanofiber and mafenide drug blank sample. Conclusion: This research successfully demonstrated the fabrication of sustained-release antibiotic nanofibers using electrospinning and three biocompatible polymers. The systematic optimization approach using Design-Expert® software proved effective in tailoring the drug release behavior of nanofibers. The developed drug delivery system holds great promise for pharmaceutical applications, particularly in improving antibiotic therapies and patient care.

Tetracycline hydrochloride loaded-alginate based nanoparticle-hydrogel beads for potential wound healing applications: In vitro drug delivery, release kinetics, and antibacterial activity

Novel hydrogel beads based on nanocomposite with outstanding antibacterial and swelling capabilities have been successfully produced as an efficient drug carrier for potential drug delivery systems in wound healing applications. The beads were characterized by Fourier transform infrared spectroscopy (FT-IR), scanning electron microscopy (SEM), and EDX-Mapping analysis. Then, using tetracycline hydrochloride (TCH) as a model drug system, they were studied in vitro for their potential efficiency as pH and temperature dependent sustained drug delivery carriers. Moreover, they were assessed in terms of porosity, swelling degree, encapsulation efficiency, and in vitro release kinetics. Beads released drugs at their highest levels under alkaline circumstances (pH = 8) and at a temperature of 39 °C, with a cumulative TCH release of 96.2 % at 36 h and in accordance with the Weibull kinetics model (R2 = 0.98). Additionally, the disc diffusion experiment demonstrated the strong antibacterial activity of the synthesized beads and offered a feasible and cost-effective wound dressing material for treating infected wounds.

Imidazole-mediated stability of block copolymer micelles and its application in drug delivery

Block copolymer micelles have emerged as a safer alternative for delivering drugs in biomedical applications. Recent studies have shown that the stability of these micelles can significantly impact the efficiency of drug delivery. Here, we propose a method to regulate the stability of block copolymer micelles by introducing a third monomer. Specifically, we synthesized the block copolymer PDPA18-b-P(Vim18-co-P(EG)5MA21) through reversible addition-cracking chain transfer (RAFT) polymerization based on PDPA19-b-P(P(EG)5MA)18. The diblock three-component copolymer is a unique copolymer, in which the hydrophilic block being doped the third monomer with pH-sensitive property, resulting in distinctive physiological properties. Both PDPA18-b-P(Vim18-co-P(EG)5MA21) and PDPA19-b-P(P(EG)5MA)18 can self-assemble into micelles with a core-shell structure. In the case of PDPA19-b-P(P(EG)5MA)18 micelles, the solvophobic PDPA19 block forms the core, while the solvophilic P(P(EG)5MA)18 block forms the shell. To regulate the stability of the block copolymer micelles, an imidazole intermediate layer with pH-responsiveness is introduced between PDPA core and P(P(EG)5MA) shell. The introduction of the imidazole monomer affect the stability of block copolymer micelles and the release kinetics of drugs. We validated that these PDPA18-b-P(Vim18-co-P(EG)5MA21) micelles exhibit higher stability under neutral conditions and show enhanced drug release in mildly acidic conditions compared to PDPA19-b-P(P(EG)5MA)18 micelles. Overall, this report demonstrates that copolymerization of imidazole monomer is a powerful approach to mediated the stability of block copolymer micelles for drug delivery applications.

EDITORIAL: PIONEERING THE FUTURE OF HEALTHCARE THROUGH ADVANCES IN NOVEL DRUG DELIVERY SYSTEMS

With great delight and anticipation, I extend my heartfelt greetings to you as we commence a new venture with the latest release of the International Journal of Pharmacy and Integrated Health Sciences (IJPIHS). This issue is particularly noteworthy as it highlights the pivotal domains of Pharmaceutical Sciences, Clinical Pharmacy, and Drug Delivery Systems, demonstrating their significant influence on applications in healthcare.
 In the ever-evolving landscape of pharmaceuticals and healthcare, the quest for innovative drug delivery systems has emerged as a pivotal force, reshaping the dynamics of patient care and treatment outcomes. This editorial aims to shed light on the ground-breaking advancements in novel drug delivery systems, as we navigate the frontiers of the pharmaceutical industry in our pursuit of improved therapeutic efficacy and patient well-being. In recent years, the field of drug delivery has witnessed a paradigm shift, driven by a convergence of interdisciplinary research, technological breakthroughs, and a deep understanding of physiological processes. The International Journal of Pharmacy and Integrated Health Sciences is proud to contribute to this ongoing dialogue by showcasing the latest research and developments in novel drug delivery systems.
 One of the key challenges in traditional drug administration lies in achieving optimal drug concentrations at the target site while minimizing side effects. Novel drug delivery systems address this challenge by providing precise control over drug release kinetics, enhancing bioavailability, and enabling targeted delivery to specific tissues or cells. This not only maximizes therapeutic effects but also minimizes adverse reactions, thereby improving patient compliance and overall treatment outcomes.
 Nanotechnology has emerged as a frontrunner in this domain, offering unprecedented opportunities for designing advanced drug delivery platforms. Nanoparticles, liposomes, and micelles provide versatile carriers for drugs, allowing for controlled release and targeted delivery. These nanocarriers not only protect the drug from degradation but also facilitate its transport across biological barriers, opening new avenues for personalized medicine and tailored treatment strategies.
 As we delve into the articles featured in this issue of the International Journal of Pharmacy and Integrated Health Sciences, we invite our readers to explore the multifaceted world of novel drug delivery systems. From cutting-edge research on nanomedicine to the implementation of smart drug delivery devices, the diverse contributions in this journal underscore the transformative potential of these innovations in reshaping the future of healthcare. I want to convey my appreciation to the readers of IJPIHS for their ongoing support and active involvement with our journal. Your commitment to staying informed and exchanging knowledge fuels our relentless pursuit of excellence. Thank you for being part of this remarkable journey.

Bioactive glass doped with zinc-based metal–organic frameworks (Zn/MOF) nanoparticles for antibiotic delivery applications

Zn-MOF/bioactive glass nanoparticles were successfully prepared using quick–alkali-modified sol–gel and tested for gentamicin drug delivery. Samples of 0 and 0.8 mol% Zn MOF contents (BG and BG/Zn MOF, respectively) were characterized using XRD, FTIR, TEM, and SEM/EDX. In addition, zeta characteristics and surface area parameters were also evaluated. Moreover, the cell viability of the prepared samples was tested against the osteosarcoma MG-63 cell line to evaluate the ability of prepared samples for bone regeneration. In addition, the antimicrobial activity of glass samples with and without antibiotics was determined against different microorganisms. Finally, the samples were loaded with gentamicin drug, and drug release profile and kinetics were studied too. XRD and FTIR results confirmed the physicochemical properties of the prepared samples. TEM results showed that particles were in the nano-sized range in both samples; however, the presence of Zn MOF increased the dispersity of particles. Both samples were bioactive, as indicated by hydroxyapatite formation on their surfaces. Cytotoxicity estimation of prepared materials exhibited their safe and nontoxic nature. BG/Zn MOF sample demonstrated prolonged drug release and excellent antimicrobial activity in comparison to BG alone. Therefore, the present study provides promising preliminary results regarding the usage of BG/Zn MOF nanoparticles loaded with gentamicin as an effective approach for bone regeneration.Graphical

Formulation and evaluation of fluconazole emulgels for potential treatment of vaginal candidiasis

Localised treatment of vaginal candidiasis could improve the therapeutic outcomes of patients with vaginal candidiasis as well as reduce drug dosage and dosing interval. The aim of the research project was to develop fluconazole emulgel formulations, and evaluate their physicochemical, drug release, antifungal, safety, and stability profile, for potential treatment of vaginal candidiasis. Xanthan gum and HPMC E5LV-based fluconazole emulgels were prepared using the spontaneous emulsification method and their physicochemical properties, drug content, drug release profile, anti-fungal activity against Candida albicans, in vivo vaginal biocompatibility and stability profile were evaluated using standard protocols. The fluconazole emulgels exhibited satisfactory properties: pH: 5.2–5.4; spreadability: 1.6–2.5 cm; apparent viscosity: 85–314 cP; zone of inhibition against Candida albicans: 22–38 mm; drug content: 91–102 %, and vaginal biocompatibility. All the studied fluconazole emulgels exhibited controlled fluconazole release over 6 h and their drug release kinetics fitted well with Korsmeyer-Peppas model. HPMC-based emulgels exhibited unsatisfactory real-time stability profile. To our knowledge, this is the first report where xanthan gum and HPMC E5LV-based fluconazole emulgels have been studied for possible treatment of vaginal candidiasis. Xanthan gum-based fluconazole emulgels are promising drug formulations that could reduce the drug dosage and dosing frequency. In addition, they could serve as alternative dosage forms to Flucos® gel.

Formulation and Characterization of Self-Microemulsifying Drug Delivery System (SMEDDS) of Sertraline Hydrochloride.

Sertraline hydrochloride is the most widely used selective serotonin reuptake inhibitor (SSRI) for the treatment of several depressive disorders. Its applicability is limited due to extensive metabolism and poor oral bioavailability of 44 %. The current research focused on improving the solubility and oral bioavailability of Sertraline by using microemulsions developed by a self-micro emulsifying drug delivery system (SMEDDS) for significant antidepressant action. SMEDDS were developed by selecting appropriate proportions of oil, surfactant, and co-solvents and out of them isopropyl myristate, tween 80 and propylene glycol were identified as best. The emulsification zone was demonstrated by a ternary phase diagram, and compatibility was confirmed with Fourier-transformed infrared spectroscopy (FT-IR). The formulated SMEDDS were characterized for robustness to dilution, globule size (GS), polydispersity index (PDI), viscosity, in-vitro dissolution and diffusion study, and drug release kinetics study. All the batches (A1-A9) passes the test and A3 was selected as an optimized batch that doesn't show phase separation, precipitation with globule size (101 nm), PDI (0.319), drug content (99.14±0.35 %), viscosity (10.71±0.02 mPa), self-emulsification time (46 sec), in-vitro drug release (98.25±0.22 %) within 8 h, release kinetics (Higuchi) and effective antidepressant in in-vitro diffusion studies. An optimized batch A3 observed circular in shape estimated by Transmission electron microscopy (TEM) and passes all the thermodynamic stability testing with loss of 0.271 mg of the drug after 90 days and showed marked antidepressant action with higher stability.

The effect of emulgel preparation on the stability of Kojic acid in the topical anti-hyperpigmentation products.

The emulgel, a novel drug delivery system, merges emulsion and gel, offering advantages like enhanced stability, precise control over drug release kinetics, and increased drug absorption compared to emulsions alone. Kojic acid (KA) demonstrates potent inhibition of the tyrosinase enzyme, a crucial player in the melanin synthesis pathway. The main objective of this experimental study is to formulate KA within an emulgel framework and assess its stability under various environmental conditions. One percent of KA emulgel and 1% simple gel, serving as the control product, were supplemented with varying concentrations of sodium metabisulfite (SMBS) for its antioxidant properties. The formulations were segregated into four groups and subjected to diverse maintenance and stress conditions over a three-month period. Monthly evaluations of physicochemical alterations were conducted, initially employing digital photography, followed by the extraction of KA and subsequent quantification of its concentration through high performance liquid chromatography (HPLC). The best formulations for retaining KA among the prepared ones were the 0.25% SMBS KA emulgel and the 0.1% SMBS KA simple gel, capable of retaining 86% and 76% of the initial KA content under stress conditions, respectively (p < 0.0001). Regarding to this study, ideal storage condition for KA emulgel and simple gel is in the refrigerator temperatures. Moreover, optimal SMBS concentrations for stability enhancement are 0.25% for emulgel and 0.1% for the simple gel. A significant statistical difference was observed between refrigerated emulgel and simple gel in the retention of KA in the presence of optimum concentration of antioxidants (p < 0.0001).

Optimization and characterization of xanthan gum based multiparticulate formulation for colon targeting

To optimize and characterize xanthan gum multi-particulate formulation for colon targeting, which increases the residence time at the absorbing surface of the colon. Xanthan gum was dispersed in cold water containing drug and was permitted to expand for 2 ​h. Sodium alginate was blended well in 10 ​ml of water. Xanthan gum solution containing the drug was added to sodium alginate solution and 0.3 ​ml of glutaraldehyde was added to the dispersion, with constant stirring. Then, polymer-drug solution was added dropwise into 5% w/v calcium chloride solution with continuous stirring, producing microspheres filtered by Whatman filter paper and dried at 30 ​°C–40 ​°C. Microspheres were performed by chemical cross-linking with glutaraldehyde, which increased the maximum drug entrapment efficiency up to 73.63 ​± ​0.65% with an increasing concentration of xanthan gum polymer 0.7% w/v for the optimized F6 batch. Better results were found by increasing the polymer concentration along with the glutaraldehyde concentration. The kinetics of drug release for the F6 batch was considered as an optimized batch because the regression value was found to be 0.997 in the peppas model. The accelerated stability study on the optimized F6 batch performed to learn whether the drug has any change during its period of usability. The polysaccharide remains intact in the stomach and intestine and the drug was released in the colon with low toxicity and biodegradability. The present studies showed that optimizing and characterizing xanthan gum multi-particulate formulation for colon targeting gives metronidazole the most effective and controlled delivery.