1-monooleoyl-rac-glycerol and Periodontitis

The current research study is based on the design and development of a sol-gel biodegradable controlled-release formulation for use in the treatment of periodontal diseases. Glycerylmonooleate (GMO) was used as a main composition in the gel base. The influence of various additives, e.g., glycerylmonostearate (GMS), methylcellulose (MC), surfactants, and triglycerides, in GMO formulations on rheologic and swelling properties and release characteristics was described. It was demonstrated that the surfactants and triglycerides affected rheologic behavior, whereas GMS and MC influenced both rheologic and swelling properties of the bases. The release study revealed that drug released from the gel bases depended on the square root of time. The kinetics can be explained by the Higuchi's diffusion theory. Some polyols could enhance drug release from the gel. The stability results suggested that the dental gels obtained should be kept in the low temperature range.

Topics: Anti-Bacterial Agents; Delayed-Action Preparations; Drug Stability; Excipients; Gels; Glycerides; Periodontitis; Rheology; Solubility; Technology, Pharmaceutical; Temperature; Tetracycline

Elyzo 25% Dentalgel (EDG) which is developed for use in the treatment of periodontitis is a suspension of metronidazole benzoate (40%) in a mixture of glyceryl mono-oleate (GMO) and triglyceride (sesame oil). Metronidazole can be detected in the periodontal pockets 24-36 h after application. The aim of the present study was to estimate the period of time that the gel matrix persists on periodontal pockets after 1 application of EDG. 12 patients were included in the study. From each patient, 1 sample was taken before and immediately after, and 1, 2, 3, 4, 5, 6, 8, 12 and 24 h after application. Subgingival scaling followed by absorption of gingival crevicular fluid with filter paper was used for sampling. The sampling unit was 1 tooth. Each sample was assayed for the amount of GMO and oleic acid (a degradation product of GMO) by means of high-performance liquid chromatography (HPLC) with UV detection. To allow determination of the GMO dose applied into the pockets and to estimate the recovery rate of the sampling method, 1 tooth in each patient was selected for sampling as soon as the gel had set, i.e., about 10 min after application. Only in 1 patient was a detectable amount of GMO within the pocket revealed 24 h after application. This amount was approximately 0.5% of the mean GMO dose applied around 1 tooth. GMO was found no longer than 12 h in the remaining patients.

Topics: Absorption; Adult; Chromatography, High Pressure Liquid; Dental Scaling; Female; Gels; Gingival Crevicular Fluid; Glycerides; Humans; Male; Metronidazole; Middle Aged; Oleic Acid; Oleic Acids; Periodontal Pocket; Periodontitis; Sesame Oil; Time Factors