ABSTRACT
Stimulus-responsive transdermal drug delivery systems can achieve specific drug release and improve drug utilization. According to the different stimulation modes， these preparations can be divided into endogenous stimulus-responsive， exogenous stimulus-responsive and combined stimulus-responsive transdermal drug delivery systems. The endogenous stimulation- responsive transdermal drug delivery system can respond specifically to changes in temperature and pH of the lesion site through carrier materials， so as to deliver drugs to the target site. Exogenous stimulus-responsive transdermal drug delivery system can use light， heat， magnetic， electric and other external stimulation to make the carrier material phase change， so as to achieve drug delivery. The combined stimulus-responsive transdermal drug delivery system is a combination of two or more stimulus-responsive percutaneous drug delivery systems， such as temperature-pH dual-responsive drug delivery system. At present， the relevant studies of stimulus-responsive transdermal drug delivery systems are mostly in the experimental stage， and further evaluation of stability， toxicity and skin irritation is needed in the future to lay a theoretical foundation for clinical application.
ABSTRACT
Paclitaxel (PTX) is a complex secondary metabolite isolated from Taxus brevifolia, which widely used as chemotherapentic agent with a broad spectrum of actinity against cancer in the world. Its water solubility was poor and oral bioavailability was low. Cremophor-EL was used in traditional PTX injections to improve the solubility of PTX, and resulted in several adverse side effects such as severe hypersensitivity. Pre-desensitization treatment was needed before clinical use. Recently, a variety of non-injection drug delivery systems (DDS) of PTX have been developed. In this paper, the research progress of non-parenteral PTX was reviewed, including oral administration systems, vaginal administration systems, transdermal DDS, implantable DDS, transdermal DDS, intranasal administration and inhalation DDS, so as to provide references for future study and clinical applications.
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OBJECTIVE: To investigate the pharmacokinetics of triptolide gels, nanoemulsions and nanoemulsion gels by simultaneous skin and blood microdialysis in rats. METHODS: The microdialysis systems include linear probes and vascular probes which are used for measuring the recovery of triptolide in skin and blood, respectively. Linear probe and vascular probe were implanted in SD rats after abdominal hair removal. Triptolide gels, nanoemulsions and nanoemulsion gels were administered to SD rats. The probe was continuously perfused with PBS(pH 7.4) at a flow rate of 3 μL•min-1. Dialysate samples were collected every 30 min and continuously performed for 12 h. The dialysis samples were determined by LC-MS. RESULTS: The AUC0-t(s) of triptolide nanoemulsions and nanoemulsion gels were significantly higher than those of triptolide gels in skin and blood. Moreover, compared with the concentration of triptolide nanoemulsions in skin and blood, triptolide was released more smoothly from nanoemulsion gels, providing a sustained release effect and an improved bioavailability. CONCLUSION: The technique of simultaneous skin and blood microdialysis is able to detect the concentration of drug in the skin and blood of rats, which provides a new method for the pharmacokinetic study of tripolide.
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The aim of this paper was to explore the effects of Frankincense and Myrrh essential oil on transdermal absorption, and investigate the mechanism of permeation on the microstructure and molecular structure of stratum corneum. Through the determination of stratum corneum/medium partition coefficient of ferulicacid in Chuanxiong influenced by Frankincense and Myrrh essential oil, the effects of volatile oil of frankincense and Myrrh on the the microscopic and molecular structure of stratum corneum were explored by observation of skin stratum corneum structure under scanning electron microscopy, and investigation of frankincense and myrrh essential oil effects on the molecular structure of keratin and lipids in stratum corneum under Fourier transform infrared spectroscopy. The results showed that the oil could enhance the distribution of ferulic acid in the stratum corneum and medium, and to a certain extent damaged the imbricate structure of stratum corneum which was originally regularly, neatly, and closely arranged; some epidermal scales turned upward, with local peeling phenomenon. In addition, frankincense and myrrh essential oil caused the relative displacement of CH2 stretching vibration peak of stratum corneum lipids and amide stretching vibration peak of stratum corneum keratin, indicating that frankincense and myrrh essential oil may change the conformation of lipid and keratin in the stratum corneum, increase the bilayer liquidity of the stratum corneum lipid, and change the orderly and compact structure to increase the skin permeability and reduce the effect of barrier function. It can be concluded that Frankincense and Myrrh essential oil can promote the permeation effect by increasing the distribution of drugs in the stratum corneum and changing the structure of the stratum corneum.
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OBJECTIVE@#To report the influence of transdermal delivery of asiatic acid (AA) in Plasmodium berghei-infected Sprague Dawley rats on physicochemical changes, %parasitaemia and associated pathophysiology.@*METHODS@#A topical once-off AA (5, 10, and 20 mg/kg)- or chloroquine (CHQ)-pectin patch was applied on the shaven dorsal neck region of Plasmodium berghei-infected Sprague Dawley rats (90-120 g) on day 7 after infection. Eating and drinking habits, weight changes, malaria effects and %parasitaemia were compared among animal groups over 21 d.@*RESULTS@#AA-pectin patch application preserved food and water intake together with %weight gain. All animals developed stable parasitaemia (15-20%) by day 7. AA doses suppressed parasitaemia significantly. AA 5 mg/kg patch was most effective. AA and CHQ displayed bimodal time-spaced peaks. CHQ patch had a longer time course to clear parasitaemia.@*CONCLUSIONS@#AA influences bio-physicochemical changes and parasitaemia suppression in dose dependent manner. In comparison by dose administered, AA has much better efficacy than CHQ. AA may be a useful antimalarial. AA and CHQ displays bimodal peaks suggesting possible synergism if used in combination therapy.
ABSTRACT
Objective To report the influence of transdermal delivery of asiatic acid (AA) in Plasmodium berghei-infected Sprague Dawley rats on physicochemical changes, %parasitaemia and associated pathophysiology. Methods A topical once-off AA (5, 10, and 20 mg/kg)- or chloroquine (CHQ)-pectin patch was applied on the shaven dorsal neck region of Plasmodium berghei-infected Sprague Dawley rats (90–120 g) on day 7 after infection. Eating and drinking habits, weight changes, malaria effects and %parasitaemia were compared among animal groups over 21 d. Results AA-pectin patch application preserved food and water intake together with %weight gain. All animals developed stable parasitaemia (15–20%) by day 7. AA doses suppressed parasitaemia significantly. AA 5 mg/kg patch was most effective. AA and CHQ displayed bimodal time-spaced peaks. CHQ patch had a longer time course to clear parasitaemia. Conclusions AA influences bio-physicochemical changes and parasitaemia suppression in dose dependent manner. In comparison by dose administered, AA has much better efficacy than CHQ. AA may be a useful antimalarial. AA and CHQ displays bimodal peaks suggesting possible synergism if used in combination therapy.
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Objective: To investigate the correlation of transdermal delivery in vitro and in vivo with Zhibitong Cataplasm. Methods: Single-chamber diffusion cell was used and sinomenine concentration was determined by HPLC in vitro. In vivo tests, W-N method was applied to calculating the cumulative absorption of concentration by plasma drug concentration in rats. And the linear regression equation was figured through the concentration of cumulative in vitro and the concentration of cumulative absorption in vivo. Results: The regression equation was Y=0.097 24 X+0.323 91, r=0.955 1 and there was a high correlation between in vitro transdermal delivery and in vivo percutaneous absorption. Conclusion: This method can be used to evaluate the correlation between in vitro and in vivo transdermal delivery.
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IPA.Skin permeation was significantly enhanced by increasing the loading concentration of OA or NMP,larger IPA amount(8%) or PG amount(20%) could inhibit the permeation of artesunate.Conclusion Oleic acid was found to be the most efficient enhancer for artesunate,10% is the most effective concentration.