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At least 19 recordsLinked to original sources
PubMed2004

Physicochemical characterization of colloidal drug delivery systems such as reverse micelles, vesicles, liquid crystals and nanoparticles for topical administration.

Topical administration of cosmetics and pharmaceuticals involves a variety of different formulations of which colloidal drug carrier systems are currently of particular interest. After a short introduction of reverse micellar solutions, liquid crystals, vesicles and nanoparticles, appropriate methods of physicochemical characterization are introduced including X-ray diffraction, laser light scattering, electron microscopy, and differential scanning calorimetry. Emphasis is laid on topical applications of the colloidal drug delivery systems (DDS) covered, with the main objective of both sustained drug release and improved stability of DDS.

Chemical Phenomena↗
PubMed1991

The effect of topical administration of indomethacin on symptoms in corneal scars and edema.

We conducted a masked randomized study of 50 patients to evaluate the effect of administration of topical indomethacin 1% suspension on symptoms in corneal scars, edema, infiltrates, and erosions. Patients with symptoms (photophobia, pain, itching, burning sensation, foreign-body sensation, and tearing) were treated with topically administered indomethacin 1% or placebo and monitored for eight weeks. The severity of the complaints was rated and the scores were evaluated (Wilcoxon rank-sum test). Of the 25 patients treated with indomethacin, 21 (84%) had improvement in symptoms and the severity of each of the symptoms was significantly decreased. Of the 25 patients treated with placebo, one (4%) had improvement in symptoms without statistical change of the severity of the symptoms. However, when the placebo-treated patients received indomethacin drops, the symptoms were significantly decreased (P less than .002). This study suggests that topical administration of indomethacin 1% may reduce ocular symptoms in patients with corneal scars, edema, or erosions.

Administration, Topical↗
PubMed1991

The effect of sodium hyaluronate on the migration of rabbit corneal epithelium. II. The effect of topical administration.

The effect of topically administered sodium hyaluronate (Na-HA) on the healing of corneal epithelial defect was investigated using rabbit eyes. The corneal epithelium was removed surgically or with iodine vapor or n-heptanol, and saline was administered to one eye as the control, and 0.1% or 0.25% Na-HA with a molecular weight of 87.3 x 10(4) to the other eye once daily. The area of epithelial defect was measured once daily before a topical administration, and the healing rate of epithelial defect was calculated. When the corneal epithelium was removed with iodine vapor, a topical administration of 0.1% or 0.25% Na-HA did not significantly accelerate the epithelial healing. But when removed surgically or with n-heptanol, the healing rates of the corneas treated with 0.25% Na-HA significantly exceeded those of the control eyes. When the epithelium was removed surgically, treatment with 0.1% Na-HA also significantly accelerated the healing. To determine why the effect of Na-HA differed in these three models with the epithelial defect, the amount of fibronectin (FN) produced by the cornea were investigated. The amount of FN produced was determined from the concentration of FN in the medium obtained after incubation of the corneo-scleral section with corneal epithelial defect, and the amount of Na-HA retained on that cornea was estimated from radioactivity detected in tears and cornea after a topical administration of 14C-labeled Na-HA (14C-Na-HA). The corneo-scleral section whose corneal epithelium had been removed surgically, or with n-heptanol, produced a significantly larger amount of FN than that whose corneal epithelium had been removed with iodine vapor. In addition, the amount of 14C-Na-HA retained on the cornea of the first or second model also significantly exceeded that on the cornea of the third model. The topical administration of Na-HA would thus appear to accelerate the healing of the epithelial defect producing a larger amount of FN or retaining a larger amount of Na-HA.

Administration, Topical↗
PubMed1989

Cyclosporine pharmacokinetics in cats following topical ocular administration.

Topical ocular administration of two forms of cyclosporine were studied in the cat. Both forms were able to produce measurable whole-blood levels capable of suppressing in vitro lymphocyte stimulation. The kinetics of cyclosporine following administration of either oral solution or cyclosporine in olive oil were variable, with peak concentrations ranging from 450 to 1033 ng/ml and 288 to 648 ng/ml, respectively. Absorption lag time ranged from 0 to 1.34 hr for oral solution, and 0.27 to 1.2 hr for cyclosporine in olive oil. The half-life of elimination ranged from 2.41 to 10.04 hr, and 3.09 to 15.75 hr, respectively. When compared with the commercially available oral solution, cyclosporine dissolved in olive oil was better tolerated during administration. Topical ocular administration of cyclosporine in cats offers a possible alternative method of treatment for individuals intolerant of oral administration. Topical ocular administration might also replace the need for intravenous administration of cyclosporine during perioperative periods or during periods of vomiting and nausea associated with rejection or other illnesses. Due to individual variation in absorption and elimination of topically applied cyclosporine, dosages in each cat must be determined by monitoring blood, plasma, or serum levels.

Administration, Topical↗
PubMed1987

Deposition of viprostol (a synthetic PGE2 vasodilator) in the skin following topical administration to laboratory animals.

1. Topical application of 14C-viprostol, a synthetic prostaglandin E2 analogue, to laboratory animals resulted in a significant depot of radioactivity in the skin at the application site in all species studied: mouse, rat, guinea pig, rabbit and monkey, with longer residence times in the larger species. 2. The location of the 14C-label in the skin in mice and monkeys was determined by microscopic autoradiography. Evaluation of the autoradiograms show rapid penetration of the drug into the skin via the hair follicles. 3. In mouse distribution of radioactivity was evident in the stratum corneum and down the hair shafts by 30 min. after dosing. By 2 h radioactivity was also observed throughout the viable epidermis; in the dermis only the hair shafts contained significant radioactivity. At 72 h after dose removal, radioactivity was evident only in the hair follicles and hair shaft. 4. In monkey the residence time of radioactivity in the skin was significantly longer than in mouse, but the general distribution pattern was similar in both species. 5. The presence of viprostol in the hair follicles and epidermal layer after topical administration is consistent with its extensive skin metabolism previously reported.

Administration, Topical↗
PubMed1999

Human aqueous and vitreous humour levels of ciprofloxacin following oral and topical administration.

PURPOSE: To assess aqueous and vitreous humour ciprofloxacin concentrations following oral and topical administration of ciprofloxacin in patients with non-inflamed cornea and an intact crystalline lens, and to compare the concentrations of the drug given by either route. METHODS: In this prospective study, 34 patients undergoing pars plana vitrectomy for various ocular pathologies were divided into two groups. Eighteen patients received 2 drops of 0.3% ophthalmic solution of ciprofloxacin every 30 min for 3 h and then every 60 min for the next 3 h, and 16 patients received a single oral dose of 1000 mg ciprofloxacin 6 h before surgery. The aqueous and vitreous humour samples were simultaneously harvested after oral or topical administration during pars plana vitrectomy to assess penetration of the drug. These samples were assayed for ciprofloxacin concentrations by a method described previously by us using high-performance liquid chromatography. RESULTS: The aqueous and vitreous humour levels of ciprofloxacin were 0.59 +/- 0.06 microgram/ml (mean +/- SEM) and 0.64 +/- 0.06 microgram/ml after oral and 0.44 +/- 0.07 microgram/ml and 0.22 +/- 0.04 microgram/ml after topical ciprofloxacin administration, respectively. Aqueous humour levels were not statistically significantly different following oral and topical administration (p = 0.069). However, the vitreous level of the drug after oral administration was significantly higher than that after topical administration (p < 0.001). CONCLUSION: Ocular bioavailability of ciprofloxacin in aqueous humour following oral and topical administration is found to be similar when the drug was applied as described above. Penetration of ciprofloxacin into vitreous humour is less than that into aqueous humour after topical administration.

Administration, Oral↗
PubMed2005

[Dexamethasone pharmacokinetics in perilymph of guinea pig after different topical administrations].

OBJECTIVE: To determine pharmacokinetics profiles of dexamethasone (DEX) in perilymph of guinea pig with different intratympanic administrations, and to provide experimental evidence for clinical choice about administration. METHOD: Two different topical administrations placing a granule gelfoam soaked with DEX (10 g/L) in the niche of round window of guinea pig and infusing tympanic bulb with DEX solution (10 g/L) were conducted. Perilymph of the scala tympani was sampled 1-6 h after administration. DEX in the samples was assayed with high-performance liquid chromatography. RESULT: The concentrations of DEX in perilymph after placing a granule gel-foam soaked with DEX in the niche of round window were significantly higher than that after intratympanic infusing. The half-life time of DEX after placing a granule gelfoam was longer. CONCLUSION: DEX could effectively penetrate round window membrane into perilymph after different intratympanic administrations, and the method of placing a granule gelfoam soaked with DEX in the niche of round window is more effective than that of intratympanic infusing.

Administration, Topical↗
PubMed1998

Penetration of ofloxacin in human aqueous and vitreous humors following oral and topical administration.

PURPOSE: To determine aqueous and vitreous humor ofloxacin levels following oral and topical application of ofloxacin in patients with noninflamed cornea and intact crystalline lens, and to compare the drug levels provided by each route. MATERIALS AND METHODS: Twenty-six patients undergoing pars plana vitrectomy for various ocular pathologies were divided into two groups. Fourteen patients received two drops of 0.3% ophthalmic solution of ofloxacin every 30 minutes for 3 hours and every 60 minutes for the next 3 hours, and 12 patients received a single oral dose of 400 mg ofloxacin 8 hours before surgery. The aqueous and vitreous humor samples were simultaneously collected after oral or topical administration during pars plana vitrectomy to assess penetration of the drug. Samples were assayed for ofloxacin concentrations by a previously described method using high-performance liquid chromatography. RESULTS: The aqueous and vitreous humor levels of ofloxacin were 1.54 +/- 0.27 microg/mL (mean +/- standard error) and 1.77 +/- 0.24 microg/mL after oral and 1.44 +/- 0.24 microg/mL and 0.37 +/- 0.05 microg/mL after topical ofloxacin administration, respectively. Aqueous humor levels were not statistically different following oral or topical administration (P > 0.8). However, vitreous level of the drug after oral administration was significantly higher than that after topical administration (P < 0.001). CONCLUSION: Ocular bioavailability of ofloxacin in aqueous humor after oral and topical administration is similar when the drug is applied as described. Penetration of ofloxacin into vitreous humor is less than that into aqueous humor following topical application. The aqueous humor levels of ofloxacin via both routes and the vitreous level of the drug after oral route exceed the minimum inhibitory concentrations for certain bacterial species that frequently cause intraocular infection.

Administration, Oral↗
PubMedDate not supplied

[Plasma and tissue concentrations of biphenylacetic acid following 1 week oral fenbufen medication and topical administration of Felbinac gel on the knee joint].

In an randomised study 30 patients were treated during one week before undergoing an elective surgery of the knee joint with 1 or 2 g respectively of 3% Felbinac gel (biphenylacetic acid gel) or oral 300 mg Fenbufen thrice daily. Biphenylacetic acid (BPAA) is the therapeutically active metabolite of the non-steroid anti-inflammatory drug Fenbufen. Plasma concentrations were measured before, during therapy and at the time of the operation. During the surgery of the knee joint specimens of synovial fluid and -membrane, of cartilage, muscle and tendons as well as of the skin and the subcutaneous fatty tissue were obtained and the BPAA concentrations measured. There was a large variance of the obtained values in all groups. It seems that mainly methodical problems are responsible for this. At the time of surgery, the plasma concentrations following oral administration were with 10,080 ng/ml 20 to 50 times higher than those after topical administration. The tissue concentrations reached 1/8 to 1/2 of the plasma concentrations. The relation of tissue concentrations to plasma concentrations of BPAA was smaller in patients treated with oral administration than in patients treated with topical administration. Therefore a partial direct penetration of Felbinac into the deeper tissue compartments can be assumed. There was no significant difference in plasma-, synovial- or tissue concentrations between the two groups treated with the topical administration. The tissue concentrations were 1 to 2 orders of magnitude lower than those after oral administration. Only in the skin the concentrations were with 9160 respectively 3830 ng/g higher than those obtained after oral application (2110 ng/g).

Administration, Oral↗
PubMed1987

Iodine absorption after topical administration.

Absorption from povidone-iodine preparations after topical administration has been reported to be negligible, but an elderly woman had increased serum iodine levels with possible metabolic complications after povidone-iodine solution was applied to decubitus ulcers.

Administration, Topical↗
PubMed1980

Epinephrine distribution after topical administration to phakic and aphakic eyes.

Not infrequently an important clinical drug is found to have side-effects far beyond those initially anticipated. Epinephrine, administered topically in the management of open-angle glaucoma, effectively lowers intraocular pressure, but it has side-effects which may be both local and systemic. As a first approach to the understanding of these widespread effects, the present studies report the specific distribution of radioactivity labeled epinephrine--after it is applied topically to one eye--in the same eye, the opposite eye, and in other certain nonocular tissues. Further, because of the existence of the clinical syndrome known as "aphakic epinephrine maculopathy," similar measurements of distribution of labeled epinephrine after topical administration are reported for aphakic eyes. Autoradiography is used to localize radioactive epinephrine specifically within tissues histologically, and radiochromatography is used to confirm specific association of radioactivity with chemically authentic epinephrine. In general, after topical administration, the exogenously administered epinephrine is taken up and stored substantially in the iris and ciliary body and to a lesser extent in the choroid in the treated eye. If the treated eye is aphakic, significantly more labeled epinephrine appears in the choroid. Far less epinephrine is found in the retina and still less in the optic nerve of the treated eye, but uptake and storage in these tissues also increases substantially in the treated eye if the eye is aphakic. Very small but definitely measurable and identifiable amounts of epinephrine also appear in the tissues of the opposite eye, again in similar proportions. There is no difference in the amount of epinephrine which appears in the opposite eye if either or both eyes are aphakic. Significant amounts of epinephrine are also seen in nonocular tissues such as those of the heart and spleen following topical administration. While these findings do not speak to the mechanism of epinephrine side-effects on the anterior eye, the posterior eye, the opposite eye, or on systemic tissues and organs, they do address the possibility that epinephrine can cause side-effects in these areas by demonstrating its localization there following topical administration. These findings have clinical implications relevant to glaucoma management, to toxic ocular syndromes such as epinephrine maculopathy in aphakia, and to toxic systemic effects of epinephrine.

Administration, Topical↗
PubMed2002

Effects of topical administration of clodronate on alveolar bone resorption in rats with experimental periodontitis.

BACKGROUND: We examined whether topical administration of a bisphosphonate clodronate could prevent alveolar bone loss in rats with experimental periodontitis. METHODS: On day 0, elastic rings were placed around the cervix of the right and left maxillary first molars (M1) to induce inflammatory periodontitis. Fifty microl of clodronate solution at a concentration of either 0 (0.9% NaCl), 20, 40, or 60 mM was injected into the subperiosteal palatal area adjacent to the interdental area between M1 and M2 on either the left or right (experimental) side on days 0, 2, 4, and 6. The contralateral side served as a control and received 0.9% NaCl solution without clodronate. The animals were sacrificed on day 7. RESULTS: Histological examination and determination of bone mineral density in the interdental alveolar bone area between M1 and M2 revealed that placement of an elastic ring caused severe vertical and horizontal bone resorption on the control side, while the topical administration of clodronate significantly prevented such alveolar bone loss. The number of osteoclasts on the experimental side was decreased compared with the control side. Furthermore, many of the osteoclasts on the experimental side were detached from the surface of the alveolar bone and had degenerated appearances, such as rounded shapes and a loss of polarity. CONCLUSIONS: These results suggest that topical administration of clodronate may be effective in preventing osteoclastic bone resorption in periodontitis.

Acid Phosphatase↗
PubMedDate not supplied

Effect of topical administration of antiinflammatory drugs to rats with adjuvant arthritis.

Oral or intramuscular administration of antiinflammatory agents produces numerous undesirable side effects. This work explores the hypothesis that topical administration of such agents directly to the site of inflammation would have beneficial antiinflammatory effects. Topical administration of steroidal and nonsteroidal antiinflammatory drugs to rats with adjuvant arthritis was as effective as oral or intramuscular administration. Peak blood levels of radioactivity following administration of equal doses of hydrocortisone-3H were considerably lower after topical administration than after oral administration.

Administration, Oral↗
PubMed2001

Comparison of tissue concentrations after intramuscular and topical administration of ketoprofen.

PURPOSE: To assess whether topical ketoprofen, which has been reported to provide analgesic effects in clinical studies, reaches predictable tissue concentrations high enough to account for the reported analgesia. Intramuscular ketoprofen was used as positive control. METHODS: Muscle and subcutaneous tissue concentrations were assessed by microdialysis. Plasma and tissue concentrations after intramuscular injection were described using a three-compartment population pharmacokinetic model. The prediction performance of the model was assessed by superimposing tissue concentrations of 12 subjects that did not participate in the present study. RESULTS: Most dialysate concentrations after topical dosing of ketoprofen (100 mg) were below the quantification limit of 0.47 ng/ml. Plasma concentrations increased slowly and reached an apparent plateau of 7-40 ng/ml at 10-12h. No decline was observed up to 16 h. Tissue concentrations after intramuscular injection (100 mg) were about 10 times higher than those after topical dosing. Tissue concentrations measured in the majority of the 12 subjects that did not participate in the present study were found within the range of two-thirds of the predicted concentrations. CONCLUSION: Predictable and cyclooxygenase-inhibiting concentrations of ketoprofen were achieved in subcutaneous and muscle tissue after intramuscular but not after topical dosing. Thus, the tissue concentrations of ketoprofen after topical administration can hardly explain the reported clinical efficacy of topical ketoprofen.

Administration, Topical↗
PubMed1986

[Combined effect of the topical administration of OK-432 with radiation on the C3H mouse fibrosarcoma (NFSa)--TCD50 and the mechanism of action].

Optimal timing of topical administration of OK-432 and TCD50 were studied using weakly immunogenic and radioresistant C3H mouse fibrosarcoma (NFSa). The mechanism of action of this combined therapy was examined histologically and electron microscopically. Topical administration of OK-432 was performed from 2 days before irradiation to 7 days after irradiation and tumor volumes on the 20th day after irradiation were compared with a control group given radiation alone. Significant difference was observed only in the group which was given OK-432 just after irradiation. The TCD50 of the combined therapy of radiation with topical administration of OK-432, 4 KE which was given just after irradiation was 64.5 Gy and that of radiation alone was 83.5 Gy. Combined therapy shifted the TCD50 curve about 20Gy to the left. Histological examination of the tumor on the 6th day after combined therapy showed marked degeneration and necrosis of tumor cells with marked infiltration of lymphocytes. These lymphocytes were electron microscopically seen surrounding not only damaged cells, but also apparently active tumor cells. We postulate the latter cells had a tendency to be degenerative. This phenomenon suggests that lymphocytes recognize as foreign these tumor cells which are apparently active but some what damaged by radiation.

Administration, Topical↗
PubMed1994

Repeated topical administration of all-trans-retinoic acid and plasma levels of retinoic acids in humans.

BACKGROUND: Vitamin A ingestion raises plasma levels of several potentially teratogenic retinoic acids (RAs) with all-trans and 13-cis configuration, but definitive data concerning the consequences of topical administration of all-trans-RA are lacking. OBJECTIVE: The study objective was to investigate the potential for inducing systemic activity after topical administration of 0.025% all-trans-RA by measuring plasma retinoid levels. METHODS: Plasma levels of all-trans-RA, 13-cis-RA, and 4-oxo-13-cis-RA were measured in four healthy subjects before, during, and after 14 daily topical applications of all-trans-RA. RESULTS: Topical administration of all-trans-RA did not significantly increase plasma levels of all-trans-RA, 13-cis-RA, and 4-oxo-13-cis-RA. Significant decreases in levels of these RAs observed during the night may reflect diurnal variations of retinoid metabolism or lowered absorption of dietary vitamin A. CONCLUSION: Diurnal and nutritional factors influence plasma levels of endogenous retinoids to a greater extent than topical administration of all-trans-RA at doses used for acne therapy, which on the basis of these results appears unlikely to induce systemic effects.

Administration, Topical↗
PubMed1991

Effects of topical administration of timolol maleate on intraocular pressure and pupil size in dogs.

Effects of topical administration of a single dose of timolol maleate on intraocular pressure (IOP) and pupil diameter were evaluated in normotensive eyes of 11 clinically normal dogs over 12 hours (7:00 AM to 7:00 PM). Mean (+/- SEM) normal IOP was 15.5 (+/- 1.1) mm of Hg and diurnal fluctuation was observed, with the highest IOP seen in the morning. Mean normal pupil diameter was 8.5 (+/- 0.3) mm. Topical treatment with 0.5% timolol resulted in reduction of IOP in the treated and nontreated eyes. Mean reduction of IOP in the treated eye was 2.5 mm of Hg, a reduction of 16.1%, with maximal reduction of 3.7 mm of Hg. Mean reduction of IOP in the nontreated eye was 1.4 mm of Hg, a reduction of 9.0%. The treated eye had reduced pupil diameter at 30 minutes after treatment, which persisted throughout the 12 hours of the study. Mean reduction of pupil diameter in the treated eye was 2.9 mm, a reduction of 34.1%. In addition, a contralateral effect on pupil diameter was seen in the nontreated eye, with mean reduction of 1.2 mm, a reduction of 14.1%. Topical administration of timolol maleate resulted in reduction of IOP and pupil diameter in treated and contralateral eyes, thus supporting the use of timolol for treatment of glaucoma in dogs. Miosis indicates possible beta-adrenergic inhibition or alpha-adrenergic activation of the sphincter muscle. beta-Adrenergic blockade would then result in miosis.

Administration, Topical↗