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OBJECTIVE: Aim of the present study was to prepare curcumin (CUR) loaded biodegradable crosslinked gelatin (GE) film to alleviate the existing shortcomings in the treatment of periodontitis. SIGNIFICANCE: Gelatin film was optimized to provide anticipated mucoadhesive strength, mechanical properties, folding endurance, and prolonged drug release over treatment duration, for successful application in the periodontitis. METHODS: The film was developed by using solvent casting technique and "Design of Experiments" approach was employed for evaluating the influence of independent variables on dependent response variables. Solid-state characterization of the film was performed by FTIR, XRD, and SEM. Further, prepared formulations were evaluated for drug content uniformity, surface pH, folding endurance, swelling index, mechanical strength, mucoadhesive strength, in vitro biodegradation, and in vitro drug release behavior. RESULTS: Solid state characterization of the formulation showed that CUR is physico-chemically compatible with other excipients and CUR was entrapped in an amorphous form inside the smooth and uniform film. The optimized film showed degree of crosslinking 51.04 ± 2.4, swelling index 138.10 ± 1.25, and folding endurance 270 ± 3 with surface pH around 7.0. Crosslinker concentrations positively affected swelling index and biodegradation of film due to altered matrix density of the polymer. Results of in vitro drug release demonstrated the capability of the developed film for efficiently delivering CUR in a sustained manner up to 7 days. CONCLUSIONS: The developed optimized film could be considered as a promising delivery strategy to administer medicament locally into the periodontal pockets for the safe and efficient management of periodontitis.
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Curcumina/química , Gelatina/química , Plásticos Biodegradables/química , Química Farmacéutica/métodos , Curcumina/farmacología , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Liberación de Fármacos/efectos de los fármacos , Excipientes/química , Humanos , Periodontitis/tratamiento farmacológico , Polímeros/químicaRESUMEN
Metronidazole (MZ) and levofloxacin (LF) are widely employed for treatment of periodontitis, but high oral dose and resistance development after long-term oral administration limit their use. The aim of this study was to alleviate shortcomings in the treatment of periodontitis by fabrication of intrapocket, biodegradable films of chitosan (CS) loaded with MZ and LF meant for inserting into periodontal pockets to treat infections. The films were developed by solvent casting technique using propylene glycol as plasticizer and glutaraldehyde as crosslinking agent. Their physical characteristics, such as drug content, surface pH, swelling index, and folding endurance, exhibited results within limit. Further, FTIR and DSC studies revealed stability of films and compatibility between drugs and excipients. SEM images of films showed the presence of free drug particles on the surface causing burst effect. In vitro release in McIlvaine buffer pH 6.6 was of sustained nature assisted by the burst effect. CS and crosslinking agent concentrations negatively affected drug release and positively affected T90 (time for releasing 90% of the drug) due to altered matrix density. In contrast, the plasticizer concentration increases membrane permeability and hence increased drug release, lowering T90. Crosslinked films demonstrated sustained release up to 7 days. The antibacterial efficacy of films was tested on Staphylococcus aureus and Escherichia coli, indicating good antibacterial activity. Clinical trials on patients proved the therapeutic efficacy of the films by a significant (p < 0.05) decrease in the clinical markers of periodontitis, i.e. gingival index, plaque index and pocket depth. Conclusively, the films of MZ and LF were successful tools for the management of periodontitis.
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Quitosano/química , Levofloxacino/química , Levofloxacino/uso terapéutico , Metronidazol/química , Metronidazol/uso terapéutico , Periodontitis/tratamiento farmacológico , Adulto , Antibacterianos/química , Antibacterianos/uso terapéutico , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Liberación de Fármacos , Escherichia coli/efectos de los fármacos , Excipientes/química , Glutaral/química , Humanos , Persona de Mediana Edad , Bolsa Periodontal/microbiología , Plastificantes/química , Método Simple Ciego , Staphylococcus aureus/efectos de los fármacos , Adulto JovenRESUMEN
The major challenge in today's world is that medical research is facing the existence of a vast number of viruses and their mutations, which from time to time cause outbreaks. Also, the continuous and spontaneous mutations occurring in the viruses and the emergence of resistant virus strains have become serious medical hazards. So, in view of the growing number of diseases, like the recent COVID-19 pandemic that has caused the deaths of millions of people, there is a need to improve rapid and sensitive diagnostic strategies to initiate timely treatment for such conditions. In the cases like COVID-19, where a real cure due to erratic and ambiguous signs is not available, early intervention can be life-saving. In the biomedical and pharmaceutical industries, nanotechnology has evolved exponentially and can overcome multiple obstacles in the treatment and diagnosis of diseases. Nanotechnology has developed exponentially in the biomedical and pharmaceutical fields and can overcome numerous challenges in the treatment and diagnosis of diseases. At the nano stage, the molecular properties of materials such as gold, silver, carbon, silica, and polymers get altered and can be used for the creation of reliable and accurate diagnostic techniques. This review provides insight into numerous diagnostic approaches focused on nanoparticles that could have been established for quick and early detection of such diseases.
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A combination of biopolymers sodium alginate and locust bean gum has been used to prepare an interpenetrating polymeric network of an anticancer drug Capecitabine by ionotropic gelation method. For the optimization 32 levels, a full factorial design was employed to examine the influence of independent factors, i.e. polymer ratio and cross-linker concentration on responses particle size and drug entrapment. The obtained optimized formulation was examined for solid-state characterization, swelling study, in vitro drug release, SRB study, oral toxicity study, in vivo pharmacokinetic and in vivo antitumor study. The results of all the studies performed were found suitable in extending the release of a short elimination half-life drug with improved bioavailability and suggesting it to be safe and effective for oral drug delivery in treating colon cancer.
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Alginatos/química , Antineoplásicos/química , Antineoplásicos/farmacología , Capecitabina/química , Capecitabina/farmacología , Galactanos/química , Mananos/química , Gomas de Plantas/química , Polímeros/química , Animales , Biopolímeros/química , Neoplasias del Colon/tratamiento farmacológico , Portadores de Fármacos/química , Sistemas de Liberación de Medicamentos/métodos , Liberación de Fármacos , Femenino , Masculino , Ratones , Ratones Endogámicos BALB C , Microesferas , Tamaño de la Partícula , Ratas , Ratas WistarRESUMEN
The research aims the development and optimization of capecitabine loaded interpenetrating polymeric network by ionotropic gelation method using polymers locust bean gum and sodium alginate by QbD approach. FMEA was performed to recognize the risks influencing CQAs. BBD was applied to study the effect of factors (polymer ratio, amount of cross-linker and curing time) on responses (particle size, % drug entrapment and % drug release). Polynomial equations and 3-D graphs were plotted to relate between factors and responses. The results of the optimized batch viz. particle size (457.92⯱â¯1.6⯵m), % drug entrapment (74.11⯱â¯3.1%) and % drug release (90.23⯱â¯2.1%) were close to the predicted values generated by Minitab® 17. Characterization techniques SEM, EDX, FTIR, DSC and XRD were also performed for the optimized batch. To study the water transport inside IPN microbeads, swelling study was done. In vitro drug release of optimized batch showed controlled drug release for 12â¯h. Pharmacokinetic study carried out following oral administration in Albino Wistar rats exhibited that optimized microbeads had better PK parameters than free drug. In vitro cytotoxicity against HT-29 cells revealed significant reduction of the cell growth when treated with optimized formulation indicating IPN microbeads as effective dosage form for treating colon cancer.
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Biopolímeros/química , Capecitabina/química , Portadores de Fármacos/química , Liberación de Fármacos , Animales , Capecitabina/sangre , Capecitabina/farmacocinética , Preparaciones de Acción Retardada , Células HT29 , Humanos , Masculino , Microesferas , Tamaño de la Partícula , Ratas , Ratas WistarRESUMEN
We have prepared tinidazole (TNZ) functionalized biodegradable chitosan (CH)/poly (ε-caprolactone) (PCL) mucoadhesive hybrid nanofiber membrane (TNZ-PCHNF) to alleviate existing shortcomings in treatment of periodontitis. Box-Behnken design was employed for evaluating influence of formulation and processing variables on quality of final formulation. Optimized nanofiber membrane was subjected to solid-state and surface characterization studies using FTIR, DSC, XRD, SEM and AFM, which revealed that TNZ was entrapped in an amorphous form inside smooth and uniform cylindrical nanofibers without any physicochemical interaction with excipients. The optimized TNZ-PCHNF membrane had a diameter of 143.55±8.5nm and entrapment efficiency of 83.25±1.8%. In vitro drug release and antibacterial study demonstrated capability of the developed nanofiber membranes for efficiently delivering TNZ in a sustained manner up to 18days, and its ability to inhibit bacterial growth, respectively. Further, reduction of contact angle (from 123.4±2.5 to 27.4±2.3) revealed that blending of CH with PCL increases hydrophilicity of the nanofiber membrane. MTT assay and CLSM study suggested that nanofiber membrane was devoid of cytotoxicity on mouse fibroblasts. Moreover, preliminary clinical trials on patients proved therapeutic efficacy of the nanofiber membrane by eliciting a significant (p<0.05) decrease in clinical markers of periodontitis.
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Quitosano/química , Electricidad , Membranas Artificiales , Nanofibras/química , Poliésteres/química , Tinidazol/química , Animales , Antibacterianos/química , Antibacterianos/farmacología , Antibacterianos/uso terapéutico , Línea Celular , Supervivencia Celular/efectos de los fármacos , Liberación de Fármacos , Humanos , Ratones , Periodontitis/tratamiento farmacológico , Staphylococcus aureus/efectos de los fármacos , Agua/químicaRESUMEN
Increased prevalence of oral diseases such as gingivitis, periodontitis and dental caries has become major health issue worldwide. Such growing incidence of periodontitis has directly affected the development of drug delivery systems and growth of the market. Since the infections are limited to periodontal pockets or oral cavity, localized intrapocket drug delivery will be more beneficial than conventional systemic administration. Advances in intrapocket technology and innovations in the field of periodontal drug delivery led to increased patent applications. Newer trends like use of mucoadhesive polymers, in situ forming gels, viscosity modifiers, plasticizers etc which can enhance intrapocket retention of drugs have gained considerable attention among researchers and industrialists. Current market is flooded with products such as Periostat, Periochip(®), Atridox(®), Arestin(®), Actisite(®), Dentomycin(®), and Elyzol(®) and generics such as metronidazole, levofloxacin, tetracycline, doxycyline and minocycline for intrapocket delivery. There is a need of novel drugs and delivery systems with better efficacy profiles than the existing compounds. Inclusion of novel technologies like films, fibers, in situ forming implants, microparticles, nanoparticles, and liposomes as intrapocket drug delivery has great potential. Development of antibiotic free drug delivery such as antiseptics, host modulators, biofilms inhibitors and antibodies has promising role in the improvement of pathogenesis of periodontitis. Further, this review deals with various innovations in drug delivery and patents related to localized intrapocket administration of medicaments in the implications of periodontitis.