1.Preparation of an oxybutynin cubsomes gel with high permeability
Lingjun ZENG ; Yurong FU ; Yuejiao KE ; Xin ZHOU
China Pharmacist 2024;27(1):17-26
Objective To develop an oxybutynin nanotransdermal formulation with high skin permeability based on cubsomes carrier.Methods The oxybutynin loaded cubsomes(OXY-CS)was prepared by ultrasonic method.Using particle size,polydispersity index and encapsulation efficiency as evaluation indexes,stirring temperature,stirring time,stirring speed,ultrasound time,ultrasound power,glycerol monooleate/poloxamer 407 ratio(GMO/F127),carrier(GMO+F127)/drug ratio and drug concentration were optimized.The effects of drug concentration,permeation promoter and gel matrix type on skin permeability were investigated using cumulative permeation and skin retention as evaluation indicators.Results The prepared OXY-CS had small particle size and high encapsulation efficiency at stirring temperature of 50℃,stirring time of 30 min,stirring speed of 1 000 r/min,ultrasound time of 10 min,ultrasound power of 100 W,GMO/F127 ratio of 2∶1,carrier/drug ratio of 3∶1 and drug concentration of 1%,respectively.OXY-CS had high cumulative penetration and skin retention at concentration ≥ 3%.The addition of a permeation promoter to OXY-CS did not increase the cumulative penetration of the drug.The skin permeability of oxybutynin cubsomes gel made with carbomer was significantly better than those of other gel matrices.Conclusion In this study,oxybutynin is made into a topical cubsomes gel,which is expected to reduce the incidence of adverse effects associated with oral administration.
2.Advances in macrophage function and its anti-inflammatory and proresolving activity and role in periodontitis development.
West China Journal of Stomatology 2017;35(4):427-432
Macrophage plays an important role in human innate immune system. It has powerful functions, such as recognition, phagocytosis, and bacteria and foreign body removal. Periodontitis, which is a chronic infectious disease characterized by gum inflammation and bone loss, is a major cause of tooth loss in adults. Several studies demonstrated that periodontal tissue destruction is caused by the host immune response defending against infections. As an important part of host immune response, macrophage is also involved in periodontitis pathogenesis. Recently, anti-inflammatory and proresolving activities of macrophage was discovered. Thus, the complex function of macrophage in the occurrence, development, and resolution of inflammation and its potential role in periodontitis were reviewed.
3.Study on preparation technology of long-acting sustained-release oral ulcer membrane based on analytic hierarchy process and orthogonal design
Xiang XU ; Xu CHEN ; Yuejiao KE ; Zhihong LIU ; Yufang CHEN ; Xin ZHOU ; Hongtao SONG
Journal of Pharmaceutical Practice 2023;41(8):501-508
Objective To prepare a sustained-release membrane with longer adhesion time and dissolution time, and compare it with the commercially available oral ulcer membrane. Method Adhesion strength, adhesion time, swelling coefficient, dissolution time, etc. were used as the inspection indicators, and a combination of single factor inspection and analytic hierarchy process were used to screen the membrane -forming materials. The dispersion method of clotrimazole, ornidazole and borneol were investigated to prevent the drug from seed out. The method of combining orthogonal experiment and analytic hierarchy process were used to optimize the dosage of CMC-Na, PVA-1788 and glycerin; and the commercial products were compared. Results Through single-factor investigation and orthogonal experiment, the optimal ratio of excipients was selected as CMC-Na∶PVA-1788∶glycerol (3∶1∶0.08). The water-insoluble component clotrimazole, ornidazole and borneol were treated by precipitation in liquid with good effect. The best method was used to prepare the membrane. The adhesion strength was 102 g. The adhesion time was 55 min. The swelling coefficient was 1 939.52. The average dissolution time was 110 min. The appearance was white and the surface was free of bubbles, soft and elastic. The membrane forming time at 60 ℃ was 300 min and the demolding effect was better which could be completely peeled off with moderate thickness. Conclusion The oral ulcer membrane developed in this method has good appearance, comfortable use, strong adhesion, long adhesion time and dissolution time, and could stay on the ulcer surface for a long time to form physical isolation, and slowly release the drug during the dissolution process, which could play the role of long-term pain relief, antibacterial, anti-inflammatory and promote healing effects on oral ulcers.