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.

Formulation and Evaluation of Chitosan-PLGA Biocomposite Scaffolds Incorporated with Quercetin Liposomes Made by QbD Approach for Improved Healing of Oral Lesions.

The current research aims to develop and evaluate chitosan-PLGA biocomposite scaffolds in combination with quercetin liposomes to accomplish the desired impact in oral lesions where pharmacotherapeutic agent treatment through circulation could only reach the low content at the target. Optimization of quercetin-loaded liposomes was carried out using 32 factorial design. The preparation of porous scaffolds comprising produced quercetin-loaded liposomes by thin-film method was carried out in the current study using a unique strategy combining solvent casting and gas foaming procedures. The prepared scaffolds were tested for physicochemical properties, in vitro quercetin release study, ex vivo drug permeation and retention research using goat mucosa, antibacterial activity, and cell migration studies on fibroblast L929 cell lines. Improved cell growth and migration were seen in the order control < liposomes < proposed system. The proposed system has been examined for its biological and physicochemical features, and it has the potential to be utilized as an efficient therapy for oral lesions.

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.

Functional Thermoresponsive Hydrogel Molecule to Material Design for Biomedical Applications.

Temperature-induced, rapid changes in the viscosity and reproducible 3-D structure formation makes thermos-sensitive hydrogels an ideal delivery system to act as a cell scaffold or a drug reservoir. Moreover, the hydrogels' minimum invasiveness, high biocompatibility, and facile elimination from the body have gathered a lot of attention from researchers. This review article attempts to present a complete picture of the exhaustive arena, including the synthesis, mechanism, and biomedical applications of thermosensitive hydrogels. A special section on intellectual property and marketed products tries to shed some light on the commercial potential of thermosensitive hydrogels.

Encapsulation of Lactic Acid Bacteria by Lyophilisation with Its Effects on Viability and Adhesion Properties.

Lactobacillus (LAB) genera are considered important functional food but are found to have a short shelf life. In this study, two LAB, Lactobacillus plantarum (Lp) and Lactobacillus rhamnosus (Lr), were isolated from sheep's milk, and whole-genome sequencing was carried out by using 16s rRNA Illumina Nextseq, the Netherlands. The LAB were encapsulated by the lyophilisation technique using different lyoprotective pharmaceutical excipients. This process was carried out using a freeze dryer (U-TECH, Star Scientific Instruments, India). Shelf-life determination was carried out by a 12-month study using the viability survival factor (Vsf). The in vitro cell adhesion technique was carried out by using the red snapper fish along with autoaggregation and cell surface hydrophobicity as vital probiotic properties. It was observed that Lp has a significantly higher (P < 0.001) Vsf of 7.2, while Lr has a Vsf of 7 (P < 0.05) when both are encapsulated with 10% maltodextrin + 5% sucrose kept at 4°C for 12 months. The result demonstrated that Lp had significantly high (P < 0.05) cell adhesion, 96% ± 1.2 autoaggregation, and 6% cell surface hydrophobicity as compared to Lr. Moreover, this study demonstrated that lyophilised LAB with lyoprotective excipients enhances shelf life without any changes in probiotic properties when kept at 4°C exhibiting all its probiotic properties.

Tailoring the properties of mPEG-PLLA nanoparticles for better encapsulation and tuned release of the hydrophilic anticancer drug.

Gemcitabine is used as a first-line drug for treating many solid tumours. However, it suffers from a major drawback of strong side effects and short plasma half-life because of degradation by enzyme when administered intravenously. Polyesters and copolyesters are the most widely used and preferred class of biodegradable polymer. In the present work, efforts have been made to prepare poly(ethylene glycol) monomethoxy ether-poly(L-lactide) (mPEG-PLLA), a biodegradable amphiphilic copolymer with a view to improve the entrapment and tuned release of hydrophilic drug gemcitabine. The different mPEG-PLLA copolymers were synthesized with the varying ratios of mPEG and characterized by different techniques namely FTIR and 1H NMR spectroscopy, solution viscosity, differential scanning calorimetry (DSC) and gel permeation chromatography (GPC). Gemcitabine-loaded nanoparticles were prepared using mPEG-PLLA copolymers by two methods i.e. nanoprecipitation and double emulsion solvent evaporation. The nanoprecipitation method showed very less entrapment and polymer solubility in the acetone-water mixture leading to uncontrolled polymer precipitation. The difficulties encountered in the nanoprecipitation method were overcome with the help of the double emulsion (w/o/w) solvent evaporation technique. It has been observed from the results that biodegradable copolymer nanoparticles protect the drug from degradation and also help in controlling the release of encapsulated drug. The properties of nanoparticles can be tailored by varying the composition of mPEG in order to get improved entrapment efficiency and desired drug release. The nanoparticles were assessed for their in vitro cytotoxicity (MTT and FACS) and cellular uptake (fluorescence microscopy) study which showed very promising results. Nanoparticles were also studied for their in vivo release after intravenous administration to Wistar albino rats, which successfully showed controlled drug release for more than 14 days.

Synthesis, characterization of thiolated karaya gum and evaluation of effect of pH on its mucoadhesive and sustained release properties.

Present study aims at synthesis and characterization of thiolated gum karaya by reacting karaya gum with 80% thioglycolic acid resulting in esterification and immobilization of thiol groups on polymeric backbone. Immobilized thiol groups were found to be 5.026 mM/g determined by Ellman's method. It was characterized by FTIR, DSC and XRD. Directly compressible tablets prepared using thiolated gum displayed more disintegration time, swelling and mucoadhesion with increase in pH of medium simulating gastric and intestinal environment than plain gum. Controlled drug release for more than 24h by Fickian diffusion following Korsemeyer-Peppas model was observed with Metoprolol Succinate as a model drug as compared to plain gum which released more than 90% of the drug within 2h. Synthesized thiomer showed no cytotoxicity determined using HepG2 cell line. According to these results, thiolated gum karaya seems to be promising excipient for the development of mucoadhesive drug delivery systems.