BACKGROUND: In recent years, mucoadhesive dosage forms due to their advantages have attracted the interest of researchers and developers. Polymeric excipients are included into the drug composition to give adhesion to the mucous membrane. AIM: The aim of this research was to select a specific brand of pharmaceutical quality polymer that is promising for inclusion in the drug formulation. METHODS: The article presents the results of studying the mucoadhesive properties of polymers on two models using mucin: By measuring the amount of adhesion and by the evaluation the sample movement speed. RESULTS: According to the combination of two indicators, the highest mucoadhesive properties were shown by the brands of hydroxypropylmethylcellulose and xanthan gum. In addition, it was noted that hydroxyethylcellulose (HEC), sodium alginate, and hydroxypropylmethylcellulose (HPMC) also have good mucoadhesive properties. Polyethylene glycols proved to have the weakest mucoadhesive properties. The negative relationship between the average molecular weight and the sample movement speed of the HEC and HPMC was established. Obtained data showed no direct influence of the polymer average molecular weight on the amount of adhesion. It was also noted that there is no strong correlation between the amount of adhesion and the sample movement speed of the experimental samples. CONCLUSION: Based on the results of the study, it was suggested that the complex influences of the physical and chemical properties of the polymer on its mucoadhesive properties.
The experiment was conducted on 10 Wistar rats, male and female, with initial body weight 270–280 g (males) and 250–260 g (females). The drug was administered using a spray cap in 10 doses of 0.1 mg at 45 min intervals. The average cumulative dose of the drug per naloxone hydrochloride was 36.6 mg/kg for males and 39.4 mg/kg for females. The animals were monitored for 2 weeks after the exposure and then euthanized by a gentle decapitation.We noticed that after each drug administration the animals showed a decrease in motor activity. During the observation period there were no animal deaths or signs of abnormalities in their general state or behavior. Beginning on day 7 a significant increase in body weight of the animals was noted in comparison with the initial data. The relative mass of the internal organs of the treated rats remained within the physiological norm.We conclude that naloxone hydrochloride after an intranasal administration at 36.6 mg/kg for males and 39.4 mg/kg for females does not cause death of animals and or have a toxic effect on their general state, does not change their protein metabolism characteristics or the appearance of the internal organs and their mass.
Thermosensitive systems based on poloxamer 407 are widely used in targeted drug delivery; however, the stability of the phase transition temperature remains insufficiently studied. This article presents the results of a study on the effect of adding polyethylene glycols (PEG) with different molecular weights and some classical gel-forming polymers on the gelation temperature of thermoreversible compositions based on poloxamer 407 in a long-term experiment. The study showed a positive effect of PEG addition with average molecular weights at concentrations of 1.5–2.0%, as well as gelling agents at a concentration below the critical gelation concentration. The proposed rheological test for studying the samples’ adhesion can give an indirect forecast of the composition adhesive rate. Based on the conducted studies, three experimental binary systems based on poloxamer 407 were selected, with the addition of HPMC 0.5%, sodium alginate 0.5%, and PEG 1500 1.5%. These systems are the most promising for the further development of in situ targeted drug delivery systems.
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