-
Journal of Biomaterials Science.... 2010The purpose of this work was to develop a novel polyurethane hydrogel system for sustained drug release, which could be used as a vaginal drug-delivery vehicle. The...
The purpose of this work was to develop a novel polyurethane hydrogel system for sustained drug release, which could be used as a vaginal drug-delivery vehicle. The blank polyurethane hydrogels were synthesized by a polyol oligomeric, a diisocyanate and a triol (used as cross-linking agent). In order to improve the swelling ability of a polyurethane hydrogel, a small amount of 1-octadecanol was added. Additionally, the structure, mechanical properties and thermal properties of polymers were assessed by FT-IR, WAXD, DSC and mechanical tests. The results show that no more than 2.5 wt% of 1-octadecanol additives is sufficient to affect the release profile without changing the structure and mechanical properties of the polyurethane hydrogels obviously. Tinidazole was chosen as a model drug, the release data of drug from polyurethane hydrogels were fitted using the Ritger-Peppas equation and the result showed that it was non-Fickian diffusion, which means that the drug release was controlled by both swollen control and diffusion control. In conclusion, our work proves that the synthesized polyurethane hydrogel modified by 1-octadecanol may be a promising sustained release drug carrier.
Topics: Administration, Intravaginal; Delayed-Action Preparations; Diffusion; Drug Delivery Systems; Fatty Alcohols; Female; Humans; Hydrogels; Pharmaceutical Vehicles; Polymers; Polyurethanes; Water
PubMed: 20233505
DOI: 10.1163/156856209X427032 -
International Journal of Pharmaceutics Nov 2010Loading 'difficult to deliver' therapeutic agents into lipid nanoparticles (LN) is an attractive means to administer them to the skin. However, employing colloidal...
Loading 'difficult to deliver' therapeutic agents into lipid nanoparticles (LN) is an attractive means to administer them to the skin. However, employing colloidal carriers to administer therapeutic agents from semi-solid preparations adds an extra dimension to the already complex process of topical drug delivery. The aim of this work was to understand how the mobility of nanoparticles influenced the delivery of a model drug when the carriers were suspended in a hyaluronic acid (HA) vehicle. Tocopheryl acetate (TA) was loaded into lipid nanoparticles (TA(LN)) that were <100 nm in size and physically stable for more than 28 days. The TA(LN) interacted with the HA polymeric chains to increase formulation macroviscosity. Nanoparticle tracking analysis confirmed that the gel hindered the TA(LN) mobility. However, deliberate manipulation of the particle mobility in the gel by varying the concentration of HA had little effect on TA delivery. Only ca. 10 μg/cm(2) of administered TA was delivered into porcine skin regardless of the vehicle characteristics and this suggested that drug release from the LN was the rate limiting step in the delivery process and not the nanoparticle-vehicle-skin interactions.
Topics: Administration, Topical; Animals; Biological Transport; Chemistry, Pharmaceutical; Drug Carriers; Drug Interactions; Gels; Hyaluronic Acid; In Vitro Techniques; Lipids; Nanoparticles; Particle Size; Permeability; Pharmaceutical Vehicles; Skin; Skin Absorption; Swine; Tocopherols; Viscosity
PubMed: 20727392
DOI: 10.1016/j.ijpharm.2010.08.012 -
Therapeutic Delivery Feb 2018We compared the performances of two different commercial products both based on betamethasone and an antibiotic but using different pharmaceutical vehicles: a polymer... (Comparative Study)
Comparative Study
AIM
We compared the performances of two different commercial products both based on betamethasone and an antibiotic but using different pharmaceutical vehicles: a polymer and lipid-enriched cream and a conventional oil-in-water emulsion.
METHODOLOGY
Evaluation was conducted on a reconstructed human epidermis model. Moreover, skin barrier properties and cutaneous hydration of the two vehicles were evaluated on 20 human healthy volunteers.
RESULTS
Overall, the polymer and lipid-enriched formulation works as a film-forming product that retains the therapeutic agent for a long time, ensuring its penetration and absorption through the skin, and promoting skin hydration.
CONCLUSION
The above characteristics are useful in the clinical setting, especially in the context of eczematous diseases with a strong xerotic component.
Topics: Administration, Cutaneous; Adult; Anti-Bacterial Agents; Betamethasone; Dermatologic Agents; Drug Combinations; Drug Compounding; Eczema; Female; Healthy Volunteers; Humans; Male; Pharmaceutical Vehicles; Skin; Skin Absorption; Water Loss, Insensible; Young Adult
PubMed: 29424289
DOI: 10.4155/tde-2017-0070 -
The Journal of Investigative Dermatology Sep 1987Clinical and in vitro evidence suggest that pretreatment of skin with a drug or vehicle can influence topical drug delivery. In this study, hairless mouse skin in...
Clinical and in vitro evidence suggest that pretreatment of skin with a drug or vehicle can influence topical drug delivery. In this study, hairless mouse skin in diffusion cells was treated for 48 h with topical applications of vehicle alone (oleic acid (OA), isopropyl myristate, octanol (OCT), dimethylformamide, propylene glycol (PG), ethylene glycol (EG), formamide), or mixtures of OA and PG, or with 5-fluorouracil (5-FU) suspensions in each of these vehicles. Twenty-four hours after removing the initially applied agent, a standard suspension of theophylline in PG was applied to the skin surface and the flux of theophylline was determined over the next 48 h. Skin pretreatment with vehicle alone increased theophylline flux 1.6-(EG) to 122-fold (OCT) over control experiments in which the skins were not pretreated. Pretreatment with nonpolar vehicles with lower solubility parameters (OA, OCT, or mixed vehicles containing one of these) had the greatest effect on subsequent theophylline flux. Pretreatment with 5-FU in various vehicles caused a subsequent increased theophylline flux similar to the effect of vehicle alone, except for pretreatment with 5-FU in vehicles which did not have much effect themselves. In those instances, theophylline fluxes up to 16-fold over the effect of those vehicles alone were observed.
Topics: Animals; Cytological Techniques; Diffusion; Mice; Mice, Hairless; Pharmaceutical Vehicles; Premedication; Skin; Theophylline; Time Factors
PubMed: 3305716
DOI: 10.1111/1523-1747.ep12471168 -
Scientific Reports May 2015Fabrication of stimuli-triggered drug delivery vehicle s is an important milestone in treating cancer. Here we demonstrate the selective anticancer drug delivery into...
Fabrication of stimuli-triggered drug delivery vehicle s is an important milestone in treating cancer. Here we demonstrate the selective anticancer drug delivery into human cells with biocompatible 50-nm diameter halloysite nanotube carriers. Physically-adsorbed dextrin end stoppers secure the intercellular release of brilliant green. Drug-loaded nanotubes penetrate through the cellular membranes and their uptake efficiency depends on the cells growth rate. Intercellular glycosyl hydrolases-mediated decomposition of the dextrin tube-end stoppers triggers the release of the lumen-loaded brilliant green, which allowed for preferable elimination of human lung carcinoma cells (А549) as compared with hepatoma cells (Hep3b). The enzyme-activated intracellular delivery of brilliant green using dextrin-coated halloysite nanotubes is a promising platform for anticancer treatment.
Topics: Actins; Aluminum Silicates; Carcinoma, Hepatocellular; Cell Line, Tumor; Cell Survival; Clay; Dextrins; Drug Carriers; Humans; Liver Neoplasms; Lung Neoplasms; Microscopy, Atomic Force; Microscopy, Electron, Transmission; Mitochondria; Nanotubes; Pharmaceutical Preparations; Quaternary Ammonium Compounds
PubMed: 25976444
DOI: 10.1038/srep10560 -
Archives of Dermatological Research 1989In a bilateral paired comparison (randomized double-blind study) 31 dermatitis patients (atopic and contact dermatitis) were tested with two ointments containing 0.0056%... (Clinical Trial)
Clinical Trial Randomized Controlled Trial
In a bilateral paired comparison (randomized double-blind study) 31 dermatitis patients (atopic and contact dermatitis) were tested with two ointments containing 0.0056% betamethasone-17-benzoate. One ointment was applied on each side of the body. The topical formulations differed in their solution capacities for the drug by a factor of about 50 (solution-type: high mutual affinity between drug and vehicle; suspension-type: low affinity). The different antiinflammatory effects were studied visually by assessing five symptoms: erythema, scaling, infiltration, lichenification, and excoriation. On the 5th day, 73% of the patients showed significant differences between the sides in favor of the suspension-type ointment (Wilcoxon test). Blanching tests on 30 volunteers confirmed the result. The in vitro drug release, however, was faster with the solution-type ointment. The efficacy of an ointment can be increased greatly, if the solution capacity for the drug is low, and thus the partition coefficient between the stratum corneum (barrier of the skin) and the vehicle is high. As long as the barrier is not damaged completely, the difference in drug release is not the determining factor for the effect.
Topics: Adolescent; Adult; Aged; Child; Dermatitis; Female; Humans; Male; Middle Aged; Ointments; Pharmaceutical Vehicles; Solubility
PubMed: 2774647
DOI: 10.1007/BF00456392 -
Revue Medicale de Liege Apr 2007This paper is concerned with the adequate use of topical corticosteroids for the treatment of scalp psoriasis. Very potent corticosteroids are indicated in all forms of... (Review)
Review
This paper is concerned with the adequate use of topical corticosteroids for the treatment of scalp psoriasis. Very potent corticosteroids are indicated in all forms of psoriasis. The vehicle itself plays a significant role in any topical treatment. The choice of the vehicle depends on its biodisponibility and cosmetic aspect. Ideally, an easy-to-use vehicle will be preferred since it improves compliance to therapy. Foams, lotions, gels, and shampoos are better accepted than creams, pomades, ointments, and other substances with high residue content.
Topics: Adrenal Cortex Hormones; Dermatologic Agents; Dosage Forms; Excipients; Gels; Humans; Ointments; Pharmaceutical Vehicles; Psoriasis; Scalp Dermatoses
PubMed: 17566388
DOI: No ID Found -
Biological & Pharmaceutical Bulletin Nov 2000We previously developed an in vivo pharmacokinetic model that accounts for the corneal diffusion in albino rabbits and predicts the concentration of beta-blockers in the...
We previously developed an in vivo pharmacokinetic model that accounts for the corneal diffusion in albino rabbits and predicts the concentration of beta-blockers in the anterior segments. The purpose of this study is to pharmacokinetically predict the ocular absorption and characterize the systemic absorption of instilled drug with ophthalmic viscous vehicle to assist in its design and evaluation. Tilisolol and carboxymethylcellulose sodium salt (CMC) were used as the model ophthalmic drug and viscous polymer, respectively. After instillation of tilisolol with CMC vehicle in rabbits, the disposition of the drug in tear fluid, aqueous humor, and plasma were determined by HPLC. The ocular and systemic absorption were analyzed by a mathematical model including a diffusion process and a two-compartment model with first-order absorption, respectively. CMC vehicle increased the area under the concentration-time curve (AUC) of tilisolol in the tear fluid and aqueous humor and slightly reduced the AUC in plasma. The concentrations of tilisolol in the aqueous humor after instillation with CMC vehicle were accurately predicted from the tear concentrations by using the in vivo ocular pharmacokinetic model. CMC vehicle improved the ocular delivery of tilisolol.
Topics: Absorption; Adrenergic beta-Antagonists; Algorithms; Animals; Aqueous Humor; Area Under Curve; Carboxymethylcellulose Sodium; Eye; Injections, Intravenous; Isoquinolines; Male; Models, Biological; Ophthalmic Solutions; Pharmaceutic Aids; Pharmaceutical Vehicles; Rabbits; Tears; Viscosity
PubMed: 11085365
DOI: 10.1248/bpb.23.1352 -
Current Eye Research May 2021Dry eye disease (DED) is a multifactorial disease of the ocular surface characterized by loss of homeostasis of the tear film and accompanied by symptoms such as ocular... (Comparative Study)
Comparative Study Review
Dry eye disease (DED) is a multifactorial disease of the ocular surface characterized by loss of homeostasis of the tear film and accompanied by symptoms such as ocular discomfort and visual disturbance. DED is one of the most common reasons for seeking medical care in the United States and across the world. Despite this, there are a limited number of pharmacologic therapies for the treatment of DED in the United States and Europe. This review examines the different pivotal trials for DED medications and the impact the vehicle in each trial.In recent clinical trials, the vehicle of the active formulation of the medication is often used as the active comparator. A literature review of published dry eye clinical trials was performed to identify the pivotal clinical trials of DED medications and to compare treatment effect and further understand the impact of the vehicle on clinical trial outcomes.The pivotal clinical trials for the currently approved treatments for dry eye have widely varying study designs. The variations include differences in inclusion criteria, outcome measures and efficacy endpoints, and whether or not the use of concomitant artificial tears is allowed. These differences make it difficult for accurate comparisons to be made between DED medications. Each trial demonstrated that the vehicle alone has some beneficial effect on signs and symptoms of dry eye disease.This review discusses the varying trial designs and vehicles used in the pivotal studies for the four approved dry eye medications in the United States and Europe, as well as novel vehicles under development and clinical trial recommendations.
Topics: Administration, Ophthalmic; Clinical Trials as Topic; Cyclosporine; Dry Eye Syndromes; Emulsions; Humans; Ophthalmic Solutions; Pharmaceutical Vehicles; Phenylalanine; Sulfones
PubMed: 33238774
DOI: 10.1080/02713683.2020.1836226 -
Journal of Pharmaceutical Sciences Jun 1979Pilocarpine release from water-in-oil emulsion ointments was studied in vitro and in vivo, using albino rabbits. Pilocarpine release from the vehicle to the ocular...
Pilocarpine release from water-in-oil emulsion ointments was studied in vitro and in vivo, using albino rabbits. Pilocarpine release from the vehicle to the ocular fluids was dependent on shear, i.e.,blinking, and the dosing system emulsifying efficiency. A mechanical shearing component was vital for correlating corneal drug penetration and the in vitro pilocarpine release pattern. Simple diffusion studies with the vehicles did not predict drug in vivo release, but the ointment systems were all superior to an aqueous pilocarpine solution. Incorporation of a mechanical shearing component to mimic blinking gave good correlation of in vitro and in vivo results. Also, increasing the vehicle emulsifying efficiency by surfactant addition decreased shear-facilitated drug release and in vivo performance. Finally, increasing the internal aqueous phase volume fraction decreased in vivo performance and was linked to the influence of effective drug concentration in the vehicle.
Topics: Animals; Aqueous Humor; Biological Availability; Chemical Phenomena; Chemistry, Physical; Emulsions; Eye; Eyelids; Male; Ointments; Pharmaceutical Vehicles; Pilocarpine; Rabbits
PubMed: 458573
DOI: 10.1002/jps.2600680619