Flaxseed Mucilage/Hydroxypropyl Methylcellulose and Sodium Alginate/Polyvinyl Alcohol Composite Bilayer Film as a Promising Drug Carrier for Periodontal Treatment.

Objectives: The present study focused on the formulation of mucoadhesive bilayer composite films for the treatment of periodontitis and evaluation of their physicochemical properties. Materials and Methods: The solvent casting technique was used to prepare films. The primary layer (D) was prepared with flaxseed and hydroxypropyl methylcellulose composite to sustain the release of doxycycline hyclate. The second layer (S) comprised sodium alginate and polyvinyl alcohol composite for faster release of clove oil. Both layers were combined to generate the bilayer film (B). All formulations were characterized further to obtain an optimized formulation. Results: Attenuated total reflection-Fourier transform infrared radiation results showed intactness of drug and clove oil in the presence of excipients. The pH of the films was compatible with the periodontal cavity and the thickness was suitable for inserting into the cavity. The immediate release layer showed faster disintegration and swelling. The content of clove oil was above 80%. The rate of swelling of the primary layer was slow and drug content complied with the United States Pharmacopoeia. Scanning electron microscope analysis revealed intact, non-porous and smooth films. Films exhibited better mechanical strength and bioadhesiveness. Clove oil was released from the immediate release layer within 10 min, and doxycycline hyclate release was retarded to a minimum of up to 8 h in the primary layer as well as the bilayer. Formulation also had a significant effect on both Escherichia coli and Staphylococcus aureus. Conclusion: In the current study, bilayers were successfully prepared and characterized. The optimized formulation can be effectively used for the treatment of periodontitis.

Optimizing fluconazole-embedded transfersomal gel for enhanced antifungal activity and compatibility studies.

Fungal infections are of major concern all over the globe, and fluconazole is the most prevalently used drug to treat it. The goal of this research work was to formulate a fluconazole-embedded transfersomal gel for the treatment of fungal infections. A compatibility study between fluconazole and soya lecithin was performed by differential scanning calorimetry (DSC). Transfersomes were formulated by a thin-film hydration technique using soya lecithin and Span 80. A central composite design was adopted to prepare different formulations. Soya lecithin and Span 80 were chosen as independent variables, and the effect of these variables was studied on in vitro drug diffusion. Formulations were evaluated for entrapment efficiency and in vitro drug diffusion. The results of in vitro drug diffusion were analyzed using the analysis of variance (ANOVA) test. Optimized formulation was prepared based on the overlay plot and evaluated by scanning electron microscopy, DSC, vesicle size, polydispersity index (PDI), zeta potential, and in vitro drug diffusion studies. An optimized formulation was loaded into xanthan gum gel base and evaluated for pH, viscosity, in vitro and ex vivo drug diffusion, and antifungal activity. DSC studies revealed compatibility between fluconazole and soya lecithin. Entrapment efficiency and in vitro drug diffusion of various formulations ranged between 89.92% ± 0.20% to 97.28% ± 0.42% and 64% ± 1.56% to 85% ± 2.05%, respectively. A positive correlation was observed between in vitro drug diffusion and Span 80; conversely, a negative correlation was noted with soya lecithin. Entrapment efficiency, particle size, zeta potential, PDI, and drug diffusion of optimized formulation were 95.0% ± 2.2%, 397 ± 2 nm, -38 ± 5 mV, 0.43%, and 81 % ± 2%, respectively. SEM images showed well-distributed spherical-shaped transfersomes. In vitro, ex vivo drug diffusion and antifungal studies were conclusive of better diffusion and enhanced antifungal potential fluconazole in transfersomal formulation.

Development and validation of a high-performance liquid chromatography method for the estimation of esomeprazole in bulk and tablet dosage form / Desarrollo y validación de un método por cromatografía líquida de alta resolución para la estimación de esomeprazol en forma de dosificación a granel y en tableta

Introducción: Se desarrolló y validó un método de cromatografía líquida de alta resolución de fase reversa exacto, simple, preciso, rápido, económico y reproducible para la estimación de esomeprazol (ESO) en forma de dosificación a granel y en tabletas. Método: La separación se llevó a cabo en columna Finepak SIL C18T-5 (250 × 4,6 mm; 5,0 µm i.d.) utilizando tampón fosfato dihidrógeno de potasio (0,025 M): ACN (20:80 v/v) y a un caudal de 1,0 ml/min. utilizando un detector UV a 302 nm con un tiempo de ejecución de 10 min. El método fue validado para exactitud de linealidad, exactitud, precisión, límite de detección (LOD), límite de cuantificación (LOQ) y robustez. Resultados: La curva de calibración estándar fue lineal con R2 = 0,995. El LOD y el LOQ obtenidos para esomeprazol fueron 0,0001 y 0,0004 µg/mL respectivamente. El método se encontró robusto para posibles cambios. Los resultados del análisis de otros parámetros también se probaron y validaron según las pautas de ICH y los estudios de recuperación confirmaron la precisión del método propuesto. Los estudios de validación mostraron que el método HPLC desarrollado es simple, reproducible, rápido, preciso y confiable. La alta recuperación y la baja desviación estándar relativa confirman la idoneidad del método desarrollado para la determinación de esomeprazol en forma de dosificación en tabletas. Conclusión: Este método puede ser utilizado como una opción más conveniente y eficiente para el análisis de esomeprazol para establecer la calidad de la sustancia durante el análisis de rutina con resultados consistentes y reproducibles. (AU)

Introduction: An accurate, simple, precise, rapid, economic and reproducible reverse-phase high-performance liq-uid chromatography method was developed and validated for the estimation of Esomeprazole (ESO) in bulk and tablet dosage form.Method: The separation was carried out on Finepak SIL C18T-5 column (250 × 4.6 mm, 5.0 μm i. d.) using potassium dihydrogen phosphate buffer (0.025M): ACN (20:80 v/v) and at a flow rate of 1.0 mL/min. using UV detector at 302 nm with a run time of 10 min. The method was validated for accuracy for linearity, accuracy, precision, limit of detection (LOD), limit of quantification (LOQ) and robustness.Results: The standard calibration curve was linear with R2 = 0.995. LOD and LOQ obtained for esomeprazole were 0.0001 and 0.0004 μg/mL respectively. The method was found robust for possible changes. Results of analysis of other parameters were also tested and validated as per ICH guidelines and recovery studies confirmed the accuracy of the proposed method. validation studies showed that the developed HPLC method is simple, reproducible, rapid, precise and reliable. The high recovery and low relative standard deviation confirm the suitability of the developed method for the determination of esomeprazole in the tablet dosage form.Conclusion: This method may be used as a more convenient and efficient option for the analysis of esomeprazole to establish the quality of the substance during routine analysis with consistent and reproducible results. (AU)

Nanosponges- Versatile Platform as Drug Carrier.

BACKGROUND: Recently, nano-drug delivery systems have become an integral part of the most novel drug delivery systems and have gained considerable importance owing to various advantages such as carriers for poorly soluble drugs, targeting molecules at the desired site, protection from degradation etc. Objective: One of the most studied areas of nanotechnology is nanosponges. The objective of this review was to extensively summarize the various strategies for the preparation, characterization and applications of nanosponges. METHODS: In the current mini-review, we conducted a systemic search of the literature and patent inventions focusing on nanosponges. The summary of the search was inclusive of various aspects of nanosponges, such as drug characteristics to be considered while incorporating in nanosponges, other crucial additives during formulation of nanosponges, methods of preparation, characterization and applications of nanosponges in pharmaceuticals. RESULTS: Nanosponges are nanocarriers for both lipophilic and hydrophilic drugs. These are prepared by different methods such as emulsion-solvent evaporation, solvent method, melting method, ultrasound assisted method etc., and all these methods were less time consuming, more economical and evaluated by sophisticated techniques available for routine analysis. These are among the most feasible alternative to address several formulation difficulties associated with the physicochemical properties of the drug. The porous nature and small particle size are vital properties of the nanosponges that contribute crucially to correcting the drawbacks of the drug. The properties of the nanosponges can be enhanced when combined with cyclodextrins. Extensive research work has been carried out in past to explore cyclodextrin based nanosponges. Besides, it is also used for smart targeting of tumors and for drug release in a sustainable pattern. Nanosponges can be prepared by simple methods. These can be tuned to release the drug by different routes so as to achieve the maximum benefits of the drug. CONCLUSION: Huge amount of research has been carried out on nanosponges as drug carrier. The method of preparation and characterization of nanosponges are quite economical and routinely available. Owing to potential benefits and probable applications, these can be used as efficient carriers for certain drugs. The authors expect that the current review will guide the investigation of the nanosponges as nanodrug delivery systems.

Improved Mucoadhesion, Permeation and In Vitro Anticancer Potential of Synthesized Thiolated Acacia and Karaya Gum Combination: A Systematic Study.

Thiolation of polymers is one of the most appropriate approaches to impart higher mechanical strength and mucoadhesion. Thiol modification of gum karaya and gum acacia was carried out by esterification with 80% thioglycolic acid. FTIR, DSC and XRD confirmed the completion of thiolation reaction. Anticancer potential of developed thiomer was studied on cervical cancer cell lines (HeLa) and more than 60% of human cervical cell lines (HeLa) were inhibited at concentration of 5 µg/100 µL. Immobilized thiol groups were found to be 0.8511 mmol/g as determined by Ellman's method. Cytotoxicity studies on L929 fibroblast cell lines indicated thiomers were biocompatible. Bilayered tablets were prepared using Ivabradine hydrochloride as the model drug and synthesized thiolated gums as mucoadhesive polymer. Tablets prepared using thiolated polymers in combination showed more swelling, mucoadhesion and residence time as compared to unmodified gums. Thiol modification controlled the release of the drug for 24 h and enhanced permeation of the drug up to 3 fold through porcine buccal mucosa as compared to tablets with unmodified gums. Thiolated polymer showed increased mucoadhesion and permeation, anticancer potential, controlled release and thus can be utilized as a novel excipient in formulation development.

A Comparative Study of Quercetin-Loaded Nanocochleates and Liposomes: Formulation, Characterization, Assessment of Degradation and In Vitro Anticancer Potential.

Quercetin, a flavonoid, has antioxidant and anti-inflammatory properties and the potential to inhibit the proliferation of cancer, but its therapeutic efficacy is lowered due to poor solubility and bioavailability. Quercetin-loaded nanocochleates (QN) were developed using a trapping method by the addition of calcium ions into preformed negatively charged liposomes (QL) prepared by a thin-film hydration method. Liposomes were optimized by varying the concentration of Dimyristoyl phosphatidyl glycerol and quercetin by applying D-optimal factorial design using Design-Expert® software. Stable rods were observed using TEM with an average particle size, zeta potential and encapsulation efficiency of 502 nm, -18.52 mV and 88.62%, respectively, for QN which were developed from spherical QL showing 111.06 nm, -40.33 mV and 74.2%, respectively. In vitro release of quercetin from QN and QL was extended to 24 h. Poor bioavailability of quercetin is due to its degradation in the liver, so to mimic in vivo conditions, the degradation of quercetin released from QL and QN was studied in the presence of rat liver homogenate (S9G) and results revealed that QN, due to its unique structure, i.e., series of rolled up solid layers, shielded quercetin from the external environment and protected it. The safety and biocompatibility of QL and QN were provenby performing cytotoxicity studies on fibroblast L929 cell lines. QN showed superior anticancer activity compared to QL, as seen for human mouth cancerKB cell lines. Stability studies proved that nanocochleates were more stable than liposomal formulations. Thus, nanocochleates might serve as pharmaceutical nanocarriers for the improved efficacy of drugs with low aqueous solubility, poor bioavailability, poor targeting ability and stability.