Characteristic Evaluation of Gel Formulation Containing Niosomes of Melatonin or Its Derivative and Mucoadhesive Properties Using ATR-FTIR Spectroscopy

Chitosan or polyvinyl pyrrolidone (PVP) were used in combination with hydroxypropyl methylcellulose (HPMC) and poloxamer 407 (P407) as gelling agents for oral drug delivery. The performance interaction with mucin of chitosan-composed gel (F1) and PVP-composed gel (F2) was compared using attenuated total reflectance–Fourier-transform infrared (ATR-FTIR) spectroscopy at controlled temperatures of 25 and 37 °C for 1 and 5 min. F1 containing niosome-entrapped melatonin or its derivatives was investigated for mucoadhesive interaction on mucosa by ATR-FTIR spectroscopy under the same conditions. The results showed that F1-treated mucin gave a significantly lower amide I/amide II ratio than untreated mucin and F2-treated mucin did within 1 min, suggesting improved rapid affinity between mucin and chitosan. The spectra of mucosa treated with F1 incorporating niosomes of melatonin or its derivatives showed peak shifts at C=O (amide I), N-H (amide II), and carbohydrate regions and an associated decrease in the amide I/amide II ratio and increase in the carbohydrate/amide II ratio. These results indicated electrostatic interaction and hydrogen bonding between chitosan and mucin on the mucosa. In conclusion, the molecular interaction between gels and mucin/mucosa detected at amide I and amide II of proteins and the carbohydrate region could lead to an improved mucoadhesive property of the gel on the mucosa.

Development of Clove Oil In Situ Gels for Buccal Mucoadhesive

Clove oil is the volatile essential oil obtained from Syzygium aromaticum. Eugenol, which is the main component, has antimicrobial, antifungal activity and antioxidant. From antiseptic activity, clove oil can be used in treatment of oral cavity infection. The aims of this research are to formulate and evaluate clove oil mucoadhesive gel for oral applications. Gel bases were prepared from Poloxamer 407 (P407). The effect of clove oil, P407 and xanthan gum on formulations were studied. Clove oil preparations were evaluated for their physicochemical properties (physical appearance, pH, viscosity, gelling capacity and gel dissolving time at 37 °C in artificial saliva). Mucoadhesive property was studied using porcine buccal mucosa. The amount of eugenol in clove oil was analyzed by gas chromatography (GC). Stability study of clove oil gel was performed under stress and room temperature conditions (1 month). The results showed that preparations containing 0% and 1% clove oil were in situ gel while those containing 3% and 5% clove oil were gel. All formulations showed good and clear physical appearance with the pH value of 5.2. The gelling capacity and gel dissolving time of more than 15 minutes in artificial saliva at 37°C was found in all preparations. They also showed mucoadhesive property. The GC results showed that the amount of eugenol in clove oil were 99.52 ± 0.51 %V/V. The preparations containing 1% clove oil showed good physical and chemical stability after storage at room temperature for 1 month. There was no significant difference in the amount of eugenol after storage (p>0.05). In conclusion, the preparations containing 20% P407 and 1% clove oil are the most appropriate formulation.

Pharmaceutical Applications of Xanthan Gum in Ophthalmic

Introduction: Ophthalmic delivery system is one of the challenging domains of formulation and development due to tear dilutions, drug loss due to lacrimal drainage, limited volume and pre-corneal barriers. Several pharmaceutical technologies are exploited in order to counter the challenges posed by ocular route such as emulsions and suspensions. But all these technologies have stability issues which lead to their limited use.Background: Among polysaccharides, xanthan gum, a natural occurring biodegradable exopolysaccharide extracted from bacterium Xanthomonas campestris is widely accepted as one of the potential polysaccharide in ophthalmic.Review Results: Xanthan gum is commonly used as an additive to various ophthalmic formulations due to its mucoadhesive property and imparting stability to various novel pharmaceutical technologies for ophthalmic. Xanthan gum also allows chemical modifications with various ligands which consequently allow controlled release, modified dissolution rate and viscoelasticity. Conclusion: In this review we are providing an insight over potential of pharmaceutical applications of xanthan gum. Also, we have discussed the scope of chemical modifications in xanthan gum with modified physicochemical properties.

Preactivated-thiolated polyacrylic acid/1-vinyl pyrrolidone nanoparticles as nicotine carriers for smoking cessation

Preactivated-thiolated AA/VP NPs improved mucoadhesive property and prolonged nicotine release to 12 h.

Formulation of Chitosan-Ethylenediaminetetraacetic Acid/Poloxamer Gel Containing Fruit’s Hull of Garcinia mangostana Extract

The purpose of this study was to develop the formulation of chitosan-ethylenediaminetetraacetic acid (EDTA)/poloxamer containing GM extract gel. The GM extract with a concentration of 0.5% wt was incorporated into a gel formulation. The physical appearance, pH, viscosity and percentage label amount of GM extract gel were performed. The in vitro antioxidant activity of gel were evaluated using (2,2-diphenyl-1-picrylhydrazyl (DPPH) method. The antibacterial activity against Staphylococcus aureus was evaluated by the zone of inhibition method. The mucoadhesive property was investigated using viscosity technique. The results illustrate that the chitosan-EDTA/poloxamer containing GM extract gel had a yellow colour of GM extract. The pH of a gel was in the range of 4.47 – 6.87. The percentage label amount of gel was in the range of 98.71 – 99.37% and the viscosity of gel were in the range of 14767 – 14784 mPa/s and 9607 – 9641 mPa/s. The TSol-Gel temperature was 35 oC. The antioxidant activities (IC50) which evaluated by DPPH method of all gel was in the range of 13.20 – 13.57 mg/ml. The zone of inhibition of gel against S.aureus was in the range of 8.17 – 10.52 mm. The chitosan-EDTA may improve the mucoadhesive property of gel. In conclusion, the chitosan-EDTA/poloxamer containing GM extract gel may have the potential for pharmaceutical and wound healing application.

QBD-BASED DEVELOPMENT AND EVALUATION OF ENTERIC COATED MUCOADHESIVE MICROCAPSULES OF AMOXICILLIN TRIHYDRATE AS A NOVEL CHRONOTHERAPEUTIC APPROACH FOR TREATMENT OF BACTERIAL INFECTIONS

Objective: The present work entails design and characterization of enteric coated mucoadhesive microcapsules loaded with amoxicillin trihydrate as a novel chronotherapeutic approaches for the treatment and management of bacterial infection.Methods: The microcapsules were prepared by solvent evaporation technique using ethyl cellulose (EC) and hydroxypropyl methylcellulose (HPMC) as rate-controlling and mucoadhesive polymers, followed by a triple coating with Eudragit L100 as enteric coating polymer. Box-Behnken statistical design (BBD) was applied for optimization of formulations containing EC, HPMCK100M and Eudragit L100 as factors for selected responses like entrapment efficiency, mucoadhesive property and drug release in 24 h. The optimized microcapsules were also characterized for particle size, drug content, swelling index, mucoadhesive strength, and in vivo antiulcer activity.Results: The optimized microcapsules exhibited good entrapment efficiency, particle size and mucoadhesive property. FT-IR studies revealed that there was no drug-polymer interaction. SEM studies revealed that microcapsules were non-aggregated, spherical in shape and smooth appearance. In vitro drug release data from microcapsules was fitted to different kinetic models to explain release profiles. The correlation coefficient (r2) value indicated that drug release followed Higuchi model. Analysis of variance (ANOVA) showed significant difference in the release of drug from all the prepared formulations at P < 0.05 level. Accelerated stability study of optimized formulation (F4) upto 6 month showed there was no change in drug content and release characteristics during storage.