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AAPS PharmSciTech May 2017Majority of breast cancers originate from epithelial cells in the duct and lobules in the breast. Current systemic treatments for breast cancer are associated with...
Majority of breast cancers originate from epithelial cells in the duct and lobules in the breast. Current systemic treatments for breast cancer are associated with significant systemic side effects, thus warranting localized drug delivery approaches. The aim of this study was to investigate the influence of hydroalcoholic vehicle on topical delivery of 4-hydroxy tamoxifen (4-HT) through the mammary papilla (nipple). The in vitro permeability of 4-HT through porcine mammary papilla was studied using different hydroalcoholic vehicles (0, 33.33, and 66.66% alcohol). Nile red was used as a model lipophilic dye to characterize the drug transport pathway in the mammary papilla. The penetration of 4-HT through the mammary papilla increased with increase in alcohol concentration in the vehicle. The solubility of 4-HT was enhanced by increasing alcohol concentration in the vehicle. On the other hand, the epidermis/vehicle partition coefficient decreased with increase in alcohol concentration. The mammary papilla served as a depot and slowly released 4-HT into the receptor medium. Highest drug penetration was observed with saturated drug solution in 66.66% alcohol, and 4-HT levels were comparable to IC value of 4-HT. Results from this study demonstrate the possibility of using mammary papilla as a potential route for direct delivery of 4-HT to the breast.
Topics: Animals; Breast Neoplasms; Drug Delivery Systems; Female; Nipples; Pharmaceutical Vehicles; Solubility; Swine; Tamoxifen
PubMed: 27506565
DOI: 10.1208/s12249-016-0608-x -
The AAPS Journal Mar 2020Medicine co-administration with food or drink vehicles is a common administration practice in paediatrics. The aims of this review were (i) to describe the current... (Review)
Review
Medicine co-administration with food or drink vehicles is a common administration practice in paediatrics. The aims of this review were (i) to describe the current recommended strategies for co-administration of paediatric medicines with food and drinks (vehicles); (ii) to compare current administration recommendations from different countries; and (iii) to obtain a global perspective on the rationale behind the choice of recommended vehicle, in the context of the physicochemical properties of the drug and formulation. This study used a defined search strategy on the practices of paediatric medicine co-administration with vehicles, recommended in a commonly used paediatric and neonatal handbook, in addition to the information previously gathered from UK formularies. Logistic regression analysis was performed to further understand the biopharmaceutical basis of the choice of recommended vehicle for medicine co-administration. Differences were identified in the type of vehicles globally recommended for medicine co-administration. Ultimately, a statistical model was developed which provided an understanding on which vehicle is recommended for use with drugs/formulations, with basis on their biopharmaceutical properties. Overall, this review highlights the areas where further information is needed to support standardised procedures and guide the recommendation of age-appropriate and acceptable vehicles for use in the co-administration of paediatric medicines. Unified requirements are needed for harmonisation of the practice of medicine co-administration with vehicles. In vitro and/or in silico tools should be developed to evaluate the potential clinical outcomes of this practice during paediatric drug development.
Topics: Administration, Oral; Adolescent; Age Factors; Beverages; Child; Child, Preschool; Drug Compounding; Eating; Formularies as Topic; Healthcare Disparities; Humans; Infant; Models, Statistical; Patient Compliance; Pharmaceutical Preparations; Practice Guidelines as Topic; Therapeutic Equivalency
PubMed: 32133550
DOI: 10.1208/s12248-020-0432-9 -
Journal of the American Academy of... Jan 1991Propylene glycol is a commonly used vehicle for topical preparations. Although it is well suited for this purpose, it is capable of producing both primary irritant skin... (Review)
Review
Propylene glycol is a commonly used vehicle for topical preparations. Although it is well suited for this purpose, it is capable of producing both primary irritant skin reactions and allergic sensitization. The literature on propylene glycol is reviewed, with particular attention to the nature of these adverse cutaneous effects. Guidelines for patients sensitive to propylene glycol are discussed.
Topics: Administration, Cutaneous; Dermatitis, Contact; Humans; Pharmaceutical Vehicles; Propylene Glycols; Skin Diseases
PubMed: 1999538
DOI: 10.1016/0190-9622(91)70018-w -
Dermatologic Clinics Jan 2006On the surface, sunscreen products are pretty simple. They consist of a delivery vehicle containing one or more sunscreen active ingredients. When applied to the skin,... (Review)
Review
On the surface, sunscreen products are pretty simple. They consist of a delivery vehicle containing one or more sunscreen active ingredients. When applied to the skin, these sunscreen actives intercept solar ultraviolet (UV) rays before they can damage the underlying skin. However, while conceptually simple, a detailed analysis reveals that sunscreen formulations are quite complex, requiring careful selection of sunscreen active and vehicle components to control multiple performance and in-use parameters.Thus, to enable a better understanding and appreciation of sunscreen products, the typical steps in formulating a sunscreen product are described. Throughout this process, the key is to apply scientific principles together with a bit of formulation art to holistically create the best sunscreen product that meets the design targets--a sunscreen product that people will use regularly and properly.
Topics: Chemistry, Pharmaceutical; Humans; Pharmaceutical Vehicles; Skin; Sunlight; Sunscreening Agents; Technology, Pharmaceutical; Ultraviolet Rays
PubMed: 16311167
DOI: 10.1016/j.det.2005.09.002 -
Journal of Endodontics Dec 2018The aim of this study was to assess the influence of antibiotic formulations (tablet/capsule [TC] or United States Pharmacopeia [USP]-grade antibiotics) and vehicles...
INTRODUCTION
The aim of this study was to assess the influence of antibiotic formulations (tablet/capsule [TC] or United States Pharmacopeia [USP]-grade antibiotics) and vehicles (water [HO] or macrogol + propylene glycol [MP]) on the cytotoxicity and pH of triple antibiotic pastes (TAPs).
METHODS
L929 fibroblasts were exposed to TAPs prepared with TC or USP-grade antibiotics mixed with HO or MP for 72 hours. Each isolated antibiotic with each vehicle, each isolated vehicle, and the culture medium were used as controls. Cytotoxicity was evaluated by 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide and neutral red assays. The pH was measured after 3 and 8 hours of immersion of the pastes in water. Data were analyzed using analysis of variance, the Bonferroni or Tukey posttests (α = 0.05), and the Pearson correlation test (α = 0.05).
RESULTS
The pastes prepared with TC were less cytotoxic than pastes prepared with USP-grade antibiotics (P < .05), and pastes with the MP vehicle were less cytotoxic than pastes with HO (P < .05). TC TAP + MP showed the lowest cytotoxicity, whereas USP-grade TAP + HO showed the highest cytotoxicity (P < .05). All TAPs showed a pH ranging from 4.64-5.20. Irrespective of the vehicle, USP-grade TAP showed a lower pH than TC TAP (P < .05). TAPs with HO had a lower pH than TAPs with MP (P < .05).
CONCLUSIONS
The vehicle and the antibiotic formulations influenced the cytotoxicity and pH of TAP. The pastes prepared with TC and MP were less acidic and less cytotoxic than the type prepared with USP-grade antibiotics and HO.
Topics: Animals; Anti-Bacterial Agents; Cell Survival; Cells, Cultured; Drug Combinations; Drug Compounding; Fibroblasts; Hydrogen-Ion Concentration; Mice; Ointments; Pharmaceutical Vehicles; Polyethylene Glycols; Propylene Glycol; Regenerative Endodontics; Root Canal Irrigants; Water
PubMed: 30477667
DOI: 10.1016/j.joen.2018.09.009 -
Dermatology Online Journal Aug 2019Topical corticosteroids are available in many vehicles. However, patients' preference for vehicles are variable and could be tailored to maximize patient adherence.... (Review)
Review
BACKGROUND
Topical corticosteroids are available in many vehicles. However, patients' preference for vehicles are variable and could be tailored to maximize patient adherence. Spray vehicles may offer, convenience, and strong efficacy.
METHODS
A literature review was conducted using keywords: clobetasol, desoximetasone, betamethasone, triamcinolone, corticosteroid, topical, spray, vehicles, treatment, and clinical trial.
RESULTS
For moderate-to-severe plaque psoriasis, 87% of subjects achieved an Overall Disease Severity (ODS) Score ≤2 at week two and 78% achieved an ODS ≤1 after four weeks with clobetasol propionate (CP) 0.05% spray compared to 17% and 3% in the control group, respectively (P<0.001). For desoximetasone 0.25% spray, 31%-53% with moderate-to-severe psoriasis achieve Physician's Global Assessment (PGA) score ≤1 at day 28 versus 5%-18% in the vehicle spray group (P<0.01). For betamethasone dipropionate 0.05% spray, 19% with mild-to-moderate plaque psoriasis achieved an Investigator's Global Assessment (IGA) score ≤1 or a 2-grade reduction in IGA versus 2.3% in vehicle group (P≤0.001). For mild-to-severe steroid responsive inflammatory dermatoses, 64% using triamcinolone acetonide 0.2% spray achieved clear or almost clear skin at day 14 (no P value reported). Adverse events including burning, irritation, and dryness were similar across all corticosteroids.
Topics: Administration, Cutaneous; Aerosols; Dermatitis; Glucocorticoids; Humans; Inflammation; Medication Adherence; Patient Preference; Psoriasis
PubMed: 31553858
DOI: No ID Found -
AAPS PharmSciTech May 2022Compatibility and in-use stability screening studies are required for dosing vehicle selection based on the FDA's guidance, "Use of Liquids and/or Soft Foods as Vehicles...
Compatibility and in-use stability screening studies are required for dosing vehicle selection based on the FDA's guidance, "Use of Liquids and/or Soft Foods as Vehicles for Drug Administration: General Considerations for Selection and In Vitro Methods for Product Quality Assessments." One of the major analytical challenges in these studies is sample preparation because extracting active pharmaceutical ingredient (API) from the drug product mixed into viscous soft-food matrices (e.g., yogurt or apple sauce) is laborious, prone to human errors, and time-consuming. Additionally, observed in-solution degradation caused by dosing vehicle ingredients causes analytical error. In our study, NIR- and Raman-based non-destructive tests have been explored and developed with drug product powder formulation prepared in dosing vehicles. A transmission Raman chemometrics model was developed and calibrated with samples varying in API content, water content, and milled extrudate particle size distribution. The method was proven to be accurate, linear, selective, and robust. Our work with non-destructive tests eases the laboratory burdens to perform in-use stability studies with dosing vehicles for all phases of development that need to cover all application scenarios of clinical preparation and usage.
Topics: Excipients; Humans; Pharmaceutical Preparations; Powders; Spectrum Analysis, Raman
PubMed: 35501618
DOI: 10.1208/s12249-022-02286-w -
Current Eye Research Sep 2009To investigate the potential toxicity of the vehicle used for triamcinolone acetonide (TA) to the cornea, lens, ciliary body, and retina of pigmented rabbits.
PURPOSE
To investigate the potential toxicity of the vehicle used for triamcinolone acetonide (TA) to the cornea, lens, ciliary body, and retina of pigmented rabbits.
METHODS
Forty chinchilla rabbits (40 eyes) were divided into four groups: group A (control group) eyes received an intravitreal injection of 0.1 ml sterile saline solution; group B eyes received 0.1 ml (1.3 mg) TA plus vehicle; group C eyes received 0.1 ml (1.3 mg) TA alone (vehicle eliminated); group D eyes received 0.1 ml vehicle only. Intraocular pressure (IOP) was measured pre-injection and at 1, 7, 14, 30, and 90 days post-injection. Scotopic and photopic electroretinograms (ERG) were examined pre-injection and 7, 30, and 90 days post-injection. Animals were sacrificed 7, 30, and 90 days post-injection. Eyes were enucleated and examined by light microscopy (LM) and electron microscopy (EM).
RESULTS
The IOP of groups B and C was higher than that of other groups on days 1, 7, and 14 post-injection (p < 0.05). ERG amplitudes of groups B and D were lower than those of other groups on days 7 and 30 post-injection (p < 0.05). Histopathological sections indicated morphologic changes in the ciliary body, lens, and retina of eyes in groups B and D.
CONCLUSIONS
Vehicle used for TA is toxic to the lens, ciliary body, and retina of pigmented rabbit eyes after injection of intravitreal TA.
Topics: Animals; Benzyl Alcohol; Carboxymethylcellulose Sodium; Ciliary Body; Cornea; Electroretinography; Eye; Female; Glucocorticoids; Injections; Intraocular Pressure; Lens, Crystalline; Male; Pharmaceutical Vehicles; Polysorbates; Rabbits; Retina; Triamcinolone Acetonide; Vitreous Body
PubMed: 19839870
DOI: 10.1080/02713680903063082 -
Acta Ophthalmologica Aug 1979The effect of 1.4% polyvinyl alcohol (PVA) vehicle and of castor oil vehicle on ocular pilocarpine concentration was studied by radioactive method in the rabbit eye....
The effect of 1.4% polyvinyl alcohol (PVA) vehicle and of castor oil vehicle on ocular pilocarpine concentration was studied by radioactive method in the rabbit eye. Statistically higher radioactivities were measured from the anterior surface structures of the eyes dropped with oily vehicle when compared to PVA vehicle at 120 min. It is concluded that the conjunctiva and the cornea serve as a drug reservoir for the longlasting drug effect observed in the literature after oily pilocarpine drops.
Topics: Animals; Castor Oil; Conjunctiva; Cornea; Eye; Ophthalmic Solutions; Pharmaceutical Vehicles; Pilocarpine; Polyvinyl Alcohol; Rabbits
PubMed: 525286
DOI: 10.1111/j.1755-3768.1979.tb00510.x -
Postgraduate Medical Journal Aug 1974A patient requiring regular haemodialysis treatment (RDT) for end stage chronic pyelonephritis, with a recurrent manic-depressive illness was successfully treated with...
A patient requiring regular haemodialysis treatment (RDT) for end stage chronic pyelonephritis, with a recurrent manic-depressive illness was successfully treated with lithium chloride by adding it to the dialysate, when other routes had failed.
Topics: Bipolar Disorder; Female; Humans; Lithium; Middle Aged; Pharmaceutical Vehicles; Pyelonephritis; Renal Dialysis
PubMed: 4464515
DOI: 10.1136/pgmj.50.586.511