ABSTRACT
In view of the longevity and innate immune escape of red blood cells, this study designed the red blood cell membrane-coated paclitaxel nanosuspension [RBC-(PTX)NS] and investigated its physicochemical properties and antitumor effect in vitro. Paclitaxel nanosuspension [(PTX)NS] was prepared by ultrasonic precipitation and then RBC-(PTX)NS by ultrasonic coating. The formulation of(PTX)NS was optimized with Box-Behnken method and indexes of particle diameter, zeta potential, and stability. The morphology, particle diameter, stability, in vitro dissolution, and antitumor effect of(PTX)NS and RBC-(PTX)NS were characterized. The results showed that the particle diameter and zeta potential were(129.38±0.92) nm and(-22.41±0.48) mV, respectively, for the optimized(PTX)NS, while(142.5±0.68) nm and(-29.85±0.53) mV, respectively, for RBC-(PTX)NS. Under the transmission electron microscope,(PTX)NS was spherical and RBC-(PTX)NS had obvious core-shell structure. RBC-(PTX)NS remained stable for 5 days at 4 ℃. The in vitro dissolution test demonstrated that the cumulative release rate of RBC-(PTX)NS reached 79% within 20 min, which was significantly higher than that(25%) of(PTX)NS(P<0.05). As evidenced by MTT assay, RBC-(PTX)NS highly inhibited the proliferation of HepG2 cells in a dose-dependent manner. The cell membrane-coated nano-preparation preparation method is simple and reproducible. It improves the solubility of PTX and endows RBC-(PTX)NS with higher stability and stronger cytotoxicity. Thus, it is a new method for the delivery of PTX via nanocrystallization.
Subject(s)
Erythrocyte Membrane , Nanoparticles/chemistry , Paclitaxel/pharmacology , Particle Size , SuspensionsABSTRACT
Three-dimensional (3D) printing,a type of rapid prototyping technology,is based on a digital model file and prints layer-by-layer using adhesive materials,such as powdered metal or plastic.3D printing has attracted much attention in the pharmaceutical field because of the various advantages,such as simple operation,good flexibility,high repeatability,wide adaptability,and more importantly,customized service.Currently,it is used in formulations of immediate release,sustained release,implants,etc.Recently,the integration of medical devices and drugs with 3D printing has been gaining popularity.This review not only summarizes the latest progress in techniques,materials,and pharmaceutical dosage forms used in drug delivery system with 3D printing,but also analyzes its advantages and limitations,with the hope of providing reference for the development and application of 3D printing technology in drug delivery.This novel drug delivery system will bring new vitality to individualized medication.
ABSTRACT
Three-dimensional(3D)printing,a type of rapid prototyping technology,is based on a digital model file and prints layer-by-layer using adhesive materials,such as powdered metal or plastic. 3D printing has attracted much attention in the pharmaceutical field because of the various advantages,such as simple operation,good flexibility,high repeatability,wide adaptability,and more importantly,customized service. Currently,it is used in formulations of imme- diate release,sustained release,implants,etc. Recently,the integration of medical devices and drugs with 3D printing has been gaining popularity. This review not only summarizes the latest progress in techniques,materials,and pharma- ceutical dosage forms used in drug delivery system with 3D printing,but also analyzes its advantages and limitations, with the hope of providing reference for the development and application of 3D printing technology in drug delivery. This novel drug delivery system will bring new vitality to individualized medication.
ABSTRACT
Topically applied traditional Chinese medicines (TCM) generally show low transdermal rates and doses, leading to weak therapeutic efficacy. Here, cataplasm of white mustard seed varnish was prepared. The effects of iontophoresis and sonophoresis on the transdermal delivery of this TCM and its anti-asthma effect were evaluated. Active components of white mustard seed, rhizoma corydalis and Radix Kansui were obtained after alcohol extraction, respectively. The volatile oil in Asarum Heterotropoides were obtained with volatile oil extraction equipment. The drug loading ratio of cataplasms was 17% (w/w). Franz cell diffusion method was used to evaluate the accumulated permeation amount and the steady-state transdermal absorption rate of sodium thiocyanate. The improvement of sonophoresis on transdermal absorption was higher than that of iontophoresis.Asthma model of guinea pigs were established. Cataplasms of white mustard seed varnish were applied on the back of guinea pigs. Iontophoresis and sonophoresis obviously promoted the transdermal absorption and enhanced anti-asthma efficacy of white mustard seed varnish cataplasms. Pathological analysis showed that iontophoresis and sonophoresis significantly alleviated inflammation. Compared with the model group, IL-4 and IgE levels in the cataplasm group, cataplasm/iontophoresis group, cataplasm/sonophoresis group decreased obviously, although the IFN-γ levels markedly increased. Moreover, the therapeutic efficacy of cataplasm/sonophoresis group was the best in all the groups, even leading to levels similar to that of healthy animals. Iontophoresis and sonophoresis are effective methods to promote transdermal absorption of cataplasms. Moreover, the effect of sonophoresis is higher than that of iontophoresis. Physical penetration improvement techniques provide a novel insight for the wide application of transdermal TCM.
ABSTRACT
Objective To investigate the therapeutic effect of curcumin in situ hydrogels for treatment of vaginal candidiasis. Methods In situ hydrogels were prepared using poloxamer 407 and 188 as the gel matrix.Gelation temperature,gelation time and rheological characteristics were determined.Mice models with vaginal candidiasis were established.The animals were divided into six groups:the healthy mice group,the model group,the positive control group(ketoconazole cream),curcumin-loaded in situ hydrogels of 0.025,0.10 and 0.20 g/ml.Before treatment and after the fourth and eighth treatments,the vaginal smears were collected and Gram-stained.The vagina washings fluid of mice were collected to determine DNA of Lactobacillus.On 8thday,the mice were sacrificed and the vaginal tissues were excised for pathological detection.Results The gelation temperature and time of in situ hydrogels were 29℃and 2′30″,respectively.Rheological profiles demonstrated that it showed good retention effect in vivo.Compared with the model group, curcumin hydrogels of 0.025,0.10 and 0.20 g/ml could inhibit the growth of Candida albicans,inhibit vaginal mucosal edema,inflam?matory hyperplasia,and decrease the expression of inflammatory factors including TNF-α(P<0.01)and IL-1β(P<0.01).Howev?er,curcumin hydrogels could not influence the growth of lactobacillus in the vagina.It indicated that curcumin hydrogels did not de?pend on lactobacillus to treat fungal vaginitis.Conclusion Curcumin in situ hydrogels could inhibit candidiasis growth,decrease ede?ma of vaginal mucosa and inflammatory hyperplasia,and reduce the expression of inflammatory factors.It provides a novel choice for the treatment of clinical vaginal candidiasis.