Development and In Vitro Characterization of Antibiotic-Loaded Nanocarriers for Dental Delivery.

The aim of this research work was to formulate and evaluate ciprofloxacin hydrochloride-loaded nanocarriers for treating dental infections and bone regeneration. Periodontal infection is associated with inflammation, soft tissue destruction, and bone loss. The objective of the study was to extract ß tricalcium phosphate (ß-TCP) from coral beach sand using the hydrothermal conversion method and load these nanocarriers with ciprofloxacin hydrochloride. The developed drug-loaded nanocarriers were evaluated for various parameters. In vitro drug-loading studies showed the highest drug loading of 71% for F1 with a drug: carrier ratio compared to plain ciprofloxacin hydrochloride gel. ß-TCP and nanocarriers were evaluated for powder characteristics and the results were found to have excellent and fair flowability. In vitro drug release studies conducted over a period of 5 days confirmed the percentage drug release of 96% at the end of 120 h. Nanocarriers were found to be effective against S. aureus and E. coli showing statistically significant antibacterial activity at (* p < 0.05) significant level as compared to plain ciprofloxacin hydrochloride gel. The particle size of ß-TCP and nanocarriers was found to be 2 µm. Fourier transform infra-red studies showed good compatibility between the drug and the excipients. Differential scanning calorimetry studies revealed the amorphous nature of the nanocarriers as evident from the peak shift. It is obvious from the XRD studies that the phase intensity was reduced, which demonstrates a decrease in crystallinity. Nanocarriers released the drug in a controlled manner, hence may prove to be a better option to treat dental caries as compared to conventional treatments.

Impact of vitamin B6 deficiency on the severity of diabetic peripheral neuropathy - A cross sectional study.

Background: Diabetic Peripheral Neuropathy is one of the most important and significantly prevalent microvascular complications of Diabetes Mellitus. Pyridoxine is a key nutrient for protecting nerve health. The objective of this research is to study the prevalence rate of pyridoxine deficiency in Diabetic neuropathy patients, to understand the correlation between various biochemical and markers of diabetic neuropathy and pyridoxine deficiency. Results: 249 patients were selected for the study based on the selection criteria participants. 51.8% prevalence of pyridoxine deficiency in Diabetic neuropathy patients. The nerve conduction velocity significantly reduced in pyridoxine deficiency cases (p < 0.05). A strong inverse relationship is observed with fasting blood sugar levels and glycated hemoglobin pyridoxine deficiency might contribute to impaired glucose tolerance. Conclusion: There also exists a strong inverse relationship with glycemic markers. Significant direct correlation is observed with nerve conduction velocity. Pyridoxine also has properties of antioxidant which may be utilized for the management of Diabetic Neuropathy.

Formulation of Intranasal Mucoadhesive Thermotriggered In Situ Gel Containing Mirtazapine as an Antidepressant Drug.

The purpose of the present work was to develop nanoemulsion-based formulations of mirtazapine for intranasal delivery using a spray actuator to target the brain for treating depression. Research on the solubility of medications in different oils, surfactants, co-surfactants, and solvents has been done. Using pseudo-ternary phase diagrams, the various ratios of the surfactant and co-surfactant mix were computed. Thermotriggered nanoemulsion was formulated using different concentrations of poloxamer 407 (i.e., 15%, 15.5%, 16%, 16.5% up to 22%). Similarly, mucoadhesive nanoemulsion using 0.1% Carbopol and water-based plain nanoemulsions were also prepared for comparative assessment. The developed nanoemulsions were analyzed for physicochemical properties, i.e., physical appearance, pH, viscosity, and drug content. Drug-excipient incompatibility was determined by Fourier transform infrared spectral (FTIR) analysis and differential scanning calorimetry (DSC). In vitro drug diffusion studies were conducted for optimized formulations. Among the three formulations, RD1 showed the highest percentage of drug release. Ex vivo drug diffusion studies were conducted on freshly excised sheep nasal mucosa with Franz diffusion cell simulated nasal fluid (SNF) for all three formulations up to 6 h, and the thermotriggered nanoemulsion (RD1) showed 71.42% drug release with 42.64 nm particle size and a poly dispersity index of 0.354. The zeta potential was found to be -6.58. Based on the above data, it was concluded that thermotriggered nanoemulsion (RD1) has great potential to be used as an intranasal gel for treating depression in patients. It can offer great benefits by reducing dosing frequency and improving bioavailability of mirtazapine by direct nose-to-brain delivery.

Solid self-nanoemulsifying drug delivery system (S-SNEDDS) of darunavir for improved dissolution and oral bioavailability: In vitro and in vivo evaluation.

The current study was aimed to investigate the potential of solid self-nanoemulsifying drug delivery system (S-SNEDDS) composed of Capmul MCM C8 (oil), Tween 80 (surfactant) and Transcutol P (co-surfactant) in improving the dissolution and oral bioavailability of darunavir. Liquid self-nanoemulsifying drug delivery systems (L-SNEDDS) were developed by using rational blends of components with good solubilizing ability for darunavir which were selected based on solubility studies, further ternary phase diagram was constructed to determine the self-emulsifying region. The prepared L-SNEDDS formulations were evaluated to determine the effect of composition on physicochemical parameters like rate of emulsification, clarity, phase separation, thermodynamic stability, cloud point temperature, globule size and zeta potential. In vitro drug release studies showed initial rapid release of about 13.3 ± 1.4% within 30 min from L-SNEDDS followed by slow continuous release of entrapped drug and reached a maximum of 62.6 ± 3.5% release at the end of 24h. The globule size analysis revealed the formation of nanoemulsion (144 ± 2.3 nm) from the optimized L-SNEDDS formulation and was physically adsorbed onto neusilin US2. In vitro dissolution studies indicated faster dissolution of darunavir from the developed S-SNEDDS with 3 times greater mean dissolution rate (MDR) compared to pure darunavir. Solid state studies concluded the presence of drug in non-crystalline amorphous state without any significant interaction of drug with the components of S-SNEDDS. Furthermore, in vivo pharmacokinetic studies in Wistar rats resulted in enhanced values of peak drug concentration (Cmax) for L-SNEDDS (2.98 ± 0.19 µg/mL) and S-SNEDDS (3.7 ± 0.28 µg/mL) compared to pure darunavir (1.57 ± 0.17 µg/mL).

Improvement in photostability of pantoprazole sodium by microencapsulation.

Pantoprazole sodium is a proton pump inhibitor used to treat peptic ulcers and gastroesophageal reflux. This drug is unstable in acid solution, in the presence of salts, as well as in UVC radiation. Hence the aim of present study was to develop microparticles that will protect the drug from degradation in gastric acid and increase its photostability. Microparticles were prepared by the solvent evaporation method using Eudragit S 100 as enteric polymer by varying drug: polymer ratios ranging from 1:1 to 1:4. The developed microparticles were characterized for surface morphology, particle size, encapsulation efficiency, and stability in acidic media. Microparticles obtained with the ratio 1:4 were spherical, had a smooth surface, and showed the highest percent entrapment of 67 ± 2.1%. Microparticles showed uniform size distribution; about 87% of microparticles were in the size range of 50 to 75 µm. In vitro dissolution studies showed no drug release in acidic media; further prolonged drug release for a period of 9 h was obtained with a 1:4 in phosphate buffer pH 7.4 following Higuchi release kinetics with regression value of 0.9896. Photodegradation studies were performed in solar light and in UV light at 254 nm and 366 nm for 7 days. The concentration of drug was determined spectrophotometrically at 290 nm. Percent degradation under solar light for pure drug was 25%, and no significant degradation was seen in drug-loaded microparticles. Degradation under UV radiation 254 nm and 366 nm was found to be 38.6% and 12.11% and 35.11% and 6.13% for pure drug and drug-loaded microparticles respectively. LAY ABSTRACT: Pantoprazole sodium is widely used in treatment of acid-related disorders and management of gastroesophageal reflux diseases. It is an acid-labile drug that degrades in the stomach at pH 1-2 and is highly unstable in UVC light. Hence the aim of research work was to improve photostability of pantoprazole and protect it from the acidic environment by loading in gastroresistant microparticles. Various batches of microparticles were prepared by the solvent evaporation method using Eudragit S 100 as an enteric polymer that solubilizes at pH 7. Developed microparticles were characterized for different parameters and the formulation showing the highest drug entrapment was selected for photodegradation studies. Photodegradation studies were performed in solar light and in UV light at 254 nm and 366 nm for 7 days. The concentration of drug was determined spectrophotometrically at 290 nm. The percent degradation under solar light for pure drug was 25% and no significant degradation was seen in drug-loaded microparticles. Degradation under UV radiation 254 nm and 366 nm was found to be 38.6% and 12.11% and 35.11% and 6.13% for pure drug and drug-loaded microparticles, respectively. Microencapsulation decreases the penetration as well as absorption of radiation, which enhances the protection of pantoprazole sodium.