Travoprost Research Articles

Travoprost Liquid Nanocrystals: An Innovative Armamentarium for Effective Glaucoma Therapy.

To date, the ophthalmic application of liquid crystalline nanostructures (LCNs) has not been thoroughly reconnoitered, yet they have been extensively used. LCNs are primarily made up of glyceryl monooleate (GMO) or phytantriol as a lipid, a stabilizing agent, and a penetration enhancer (PE). For optimization, the D-optimal design was exploited. A characterization using TEM and XRPD was conducted. Optimized LCNs were loaded with the anti-glaucoma drug Travoprost (TRAVO). Ex vivo permeation across the cornea, in vivo pharmacokinetics, and pharmacodynamic studies were performed along with ocular tolerability examinations. Optimized LCNs are constituted of GMO, Tween® 80 as a stabilizer, and either oleic acid or Captex® 8000 as PE at 25 mg each. TRAVO-LNCs, F-1-L and F-3-L, showed particle sizes of 216.20 ± 6.12 and 129.40 ± 11.73 nm, with EE% of 85.30 ± 4.29 and 82.54 ± 7.65%, respectively, revealing the highest drug permeation parameters. The bioavailability of both attained 106.1% and 322.82%, respectively, relative to the market product TRAVATAN®. They exhibited respective intraocular pressure reductions lasting for 48 and 72 h, compared to 36 h for TRAVATAN®. All LCNs exhibited no evidence of ocular injury in comparison to the control eye. The findings revealed the competence of TRAVO-tailored LCNs in glaucoma treatment and suggested the potential application of a novel platform in ocular delivery.

RETRACTED: Travoprost-loaded PEGylated solid lipid nanoparticle-laden silicone contact lens for managing glaucoma

Conventional methods of soaking contact lenses (CLs) using drug-packaging solutions to load hydrophobic drugs, such as travoprost (TP), result in low drug loading and high burst release, along with changes in the critical properties of the lens. In this study, as a substitute for eye drop therapy, travoprost-loaded PEGylated solid lipid nanoparticles (TP-pSLNs) were used to improve the drug loading capacity of contact lenses (TP-pSLN-CLs), while also sustaining ocular drug delivery to prolong the anti-glaucoma effect. The pSLNs were spherical in shape with an average hydrodynamic diameter of 221–257 nm and a zeta potential ranging from −27.3 to −20.4 mV. The pSLNs led to improved swelling, optical transmittance, and protein adherence of the CLs compared to the non-PEGylated SLN congeners (TP-SLNs-CL) and conventional soaked lens (SM-TP-CL). The SM-TP-CL lens showed low travoprost uptake, high burst release, and a short release duration of up to 48 h. The TP-SLN-CL and TP-pSLN-CL lenses showed high drug uptake and sustained release for up to 144 h and 120 h, respectively. Although PEGylation increased the drug loading capacity, the release rate was high in the initial hours. Based on histopathological analysis, TP-pSLN-CLs were found to be safe and did not induce ocular irritation. In the rabbit tear fluid model, the TP-pSLN-20%CL batch showed high drug concentration at all time points up to 120 h compared to the SM-TP-CL (48 h) and eye drop solution (2 h). In conclusion, by using the soaking method, pSLNs improved the travoprost loading/uptake in the contact lens and improved the in vitro and in vivo results for better clinical outcomes in glaucoma treatment.

Design and evaluation of mucoadhesive in situ liposomal gel for sustained ocular delivery of travoprost using two steps factorial design

Travoprost (TRAVO) is a prostaglandin analog used to reduce the intraocular pressure (IOP) for patients suffering from glaucoma and ocular hypertension. The aim of the present study was the development of a novel in situ mucoadhesive ocular liposomal gel to prolong and improve therapeutic efficacy of TRAVO. With this purpose, liposomal formulations were prepared by implementing a full factorial design to study the effect of three factors; type of permeation enhancer (PE), PE concentration and the ratio of lecithin: cholesterol at two levels. The evaluated responses were entrapment efficiency (EE), vesicle size (VS), polydispersibility (PDI) and zeta potential (ZP). L6 (selected liposomal formulation), composed of 20% sodium deoxycholate (Na DOC) and lecithin: cholesterol at 4:1 ratio showed high EE (67.55%), suitable Ps and PDI (74.19 nm and 0.433) and ZP (−75.5 mv). L6 was incorporated in a second 31 × 21 design to study the effect of concentration of gellan gum (at three level) and carbopol 934 (at two levels) to develop in situ mucoadhesive gel. Selected liposomal in situ gel LISG2 (0.25% gellan gum and 0.5% carbopol 934), showed minimum release (18.2%) after 30 min and maximum release after 24 h (72.5%) and achieve maximum viscosity (4445cps) at physiological conditions, mucoadhesive force (0.438 N), with minimum viscosity (124 cps) at normal conditions. Selected LISG2 will be further in vivo evaluated for irritation and pharmacokinetic. TRAVO LISG was non irritant and showed improved bioavailability (higher concentration of TRAVO in aqueous humor) when compared to the marketed product, and showed more prolonged effect compared to liposomal formulation.

Comparison of the effectiveness and safety of travoprost and latanoprost for the management of open-angle glaucoma given as an evening dose.

As intraocular pressure (IOP) is primarily higher in the morning, an evening dose of prostaglandin analogs is typically used as monotherapy to decrease IOP in patients with open-angle glaucoma. Travoprost (TV) has reported efficacy in treating open-angle glaucoma; however, the safety and efficacy may be different compared with that for latanoprost (LT). The aim of the present study was to compare the effectiveness and safety of an evening dose of TV compared with that of LT in treating open-angle glaucoma. Data including IOP, results of lid and slit-lamp examination and ophthalmoscopy, as well as adverse effects in 250 affected eyes from patients with open-angle glaucoma who received either TV (n=89) or LT (n=161) once in the evening for 3-months were included in the analyses. At the end of treatment, TV (23.45±1.52 vs. 19.15±1.01 mmHg; P<0.0001) and LT (23.93±2.11 vs. 19.45±1.11 mmHg; P<0.0001) successfully lowered the IOP. In addition, there was no significant difference in the reduction of IOP values at the end of treatment between the two groups (P=0.120). Furthermore, there were no adverse effects on visual acuity (P>0.05), except for non-visual acuity, for example hyperemia (P<0.0001 for both groups), while there was a significant increase in the number of patients with dry eyes receiving TV (P=0.020) and a significant increase with eyelid swelling (P=0.036) and headache (P=0.037) in patients receiving LT. In conclusion, evening doses of TV and LT had the same efficacy and manageable adverse effects in the treatment of open-angle glaucoma (level of evidence, 3).

Development and Validation of Novel Spectro- Chemometric, Chemometric and TLC-Densitometric Methods for Simultaneous Determination of Timolol and Travoprost in their Bulk Powders and Pharmaceutical Formulation

Simple, sensitive and reliable spectro-chemometric, Chemometric and thin layer chromatography (TLC)-densitometric methods were developed for simultaneous determination of binary mixture of timolol (TIM) and travoprost (TRA) without prior separation in their bulk drugs and dosage forms. The speectro-chemometric methods used are derivative spectrophotometry and isosbestic point methods.

Synchronized Separation of Timolol from Some Prostaglandin Analogs (Bimatoprost, Latanoprost and Travoprost) for Determination in their Combined Pharmaceutical Formulations Using RP-HPLC

A rapid, precise and selective RP-LC method was developed for the simultaneous determination of the well-known beta blocker, Timolol (TIM), along with some of the most commonly prescribed prostaglandin analogues, namely; Bimatoprost (BIM), Latanoprost (LAT) and Travoprost (TRV), in laboratory prepared mixtures and in their combined pharmaceutical formulations. The chromatographic separation was carried out using gradient elution mode with a mobile phase consisting of 25 mM phosphate buffer (pH 3 ± 0.1), acetonitrile and methanol at a flow rate of 1 mL/min on a stationary phase composed of Thermo Hypersil BDS C18 (4.6×250 mm, 5 μm) column. UV detection was carried out at 295 nm and 210 nm wavelength gradient at 25°C. The method was validated according to ICH guidelines. Linearity, accuracy and precision results were satisfactory over the concentration ranges of 10.00-600.00 μg/ml for TIM and 1.00-60.00 μg/ml for BIM, LAT and TRV. The correlation coefficients (r2 values) were 0.9965 for TIM, 0.99995 for BIM, 0.99998 for LAT and 0.99996 for TRV. The method was successfully applied for the determination of TIM in its synthetic mixture and co-formulated eye drops with each of the three prostaglandin analogues BIM, LAT or TRV. The developed method is specific and accurate for the quality control and routine analysis of the cited drugs in their pharmaceutical preparations. This method is considered global and can be applied to all prostaglandin analog combinations with TIM.

Comparison of the ocular surface changes following the use of two different prostaglandin F2α analogues containing benzalkonium chloride or polyquad in rabbit eyes

Objective: The aim of this study is to compare the effect of prostaglandin analogues preserved with either 0.015% or 0.001% benzalkoium chloride (BAK); or 0.001% polyquad (PQ) on the ocular surface of rabbit eyes.Methods: Forty white rabbits were randomized to receive four-times daily instillation of either 0.0015% tafluprost (TF) preserved with 0.001% BAK (TF-BAK); 0.004% travoprost (TR) with 0.015% BAK (TR-BAK) or 0.001% PQ (TR-PQ); or preservative-free artificial tears in one eye for a 4-week period. Tear samples collected from the 40 rabbits were analyzed by enzyme-linked immunosorbent assays (ELISA) to identify the presence of inflammatory cytokines: interleukin (IL)-1β and IL-6 on day 14. Subsequently, harvested cornea and bulbar conjunctiva were evaluated using light and transmission electron microscopy (TEM).Results: IL-6 was significantly increased in TF-BAK and TR-BAK groups compared to controls and TR-PQ group (p = 0.005); however, IL-1β level was not significantly different among four groups (p = 0.360). Rabbits treated with TR-BAK showed decreased goblet cell density of bulbar conjunctiva and increased pyknotic change and vacuolization of corneal epithelial cells on light microscopy; similar change occurred but was less severe in TF-BAK group. The TR-PQ group showed similar results as the controls. The destruction of the microvillar architecture of bulbar conjunctiva and cornea was most prominent in the TR-BAK group.Conclusions: Preservatives included in the anti-glaucoma eye-drops showed different ocular surface changes according to the concentration and type in the rabbits. Prostaglandin analogues preserved with higher level of BAK may cause more harmful effects on the ocular surface than PQ-preserved medications.

Efficacy and safety of travoprost 0.004% compared with tafluprost 0.0015% in patients with primary open-angle glaucoma

Background: This prospective, open, randomized, parallel-group, comparative study is to evaluate the efficacy and side-effect profile of travoprost (TRAV) 0.004% compared with tafluprost (TAF) 0.0015% in patients with primary open-angle glaucoma (POAG) over 12 weeks. A total of 80 patients of POAG selected and were randomized to either TRAV or TAF monotherapy administered once daily in the evening for 12 weeks. Methods: The study was conducted on 80 cases of POAG, in which patients were randomized to either TRAV or TAF monotherapy administered as 1 drop daily in the evening for 12 weeks. Intraocular pressure (IOP) was measured (8 am, 12 noon and 4 pm) at each visit, slit-lamp bio-microscopy was done and side effects noted. Results: The mean IOP reduction in TRAV group decreased from 27.58±2.30 to 19.03±2.326 thus resulting in fall of 8.55 (31.0%) and in TAF group it decreased from 27.38±2.676 to 20.58±2.827 resulting in fall of 6.8 mm Hg (24.8%) was significant (p&lt;0.05). In both treatment groups, the most frequently reported adverse event at 12 weeks was red eye, noted in, 9 (22.5%) and 7 (17.5%) cases of TRAV and TAF groups respectively, though the difference was not statistically significant. Conclusion: TRAV 0.004% monotherapy produced lower diurnal IOP than TAF 0.0015% in patients with POAG and exhibited a similar safety profile.

A clinical study of Travoprost and Timolol in treating patients with primary open angle glaucoma

Objective To compare the effect of Travoprost and Timolol in treating patients with primary open angle glaucoma.Methods Using randomized,parallel group control study and choosing patients with primary open angle glaucoma (POAG),0.004％ Travoprost was applied once a day (7:00PM) in 58 patients of the experiment group and 0.5％ Timolol (7:00AM&7:00PM) in 30 patients of the control group for 1 year.Intraocular pressure (IOP),visual field and adverse reaction were observed.Results The IOP in the experiment group decreased 8.21±3.44mmHg and the visual field score reduced 0.45±1.10,the reduction in the control group was 5.44±l.78mmHg and the score increased 0.47±1.01.Visual field score of the two groups were stable.Conclusions Comparing with Timolol,Travoprost is more effective and stable in reducing IOP in patients with POAG. Key words: Travoprost; Timolol; Glaucoma

Pilot study on hypotensive effect of combination of 0.004％ travoprost with 2％ pilocarpine on normal albino rabbit

Background It has been clarified that topical administration of cholinomimetic drug or prostaglandin analogus can effectively low intraoeular pressure (IOP) in primary angle-closure glaueoma and angleopen glaucoma,respectively.The two eyedrops are often combined clinically to treat glaueomatous eye.But their effect mechanism on ciliary muscle is different.It is neeessarv to prove the clinical efficacy of combination of these two drugs.Objective This study attempted to compare hypotensive effect of individual and combinative use of 2％piloearpine and 0.004％ travoprost in normal rabbit eyes.Methods Thirty normal albino rabbits were randomly divided into three parallel groups.Lateral eye of each rabbit was appointed as the experimental eye and the fellow eye was used as control eye.2％ Pilocarpine eyedrop was instilled three times daily and 0.004％ travoprost eyedrops was used once per night in the pilocarpine and travoprost group.These two drugs were combined in the combination group.The normal saline solution was used in the control eyes IOP was measured bilaterally with Perkins application tonometer at 8:00 am on the day before and 1,2,4,8,14,24 days after the administration of eyedrops.The use of the animals complied with the Regulations for the Administration of Affairs Concerning Experimental Animals by State Science and Technology Commission.Results The IOP was significantly lower on 1 day after use of eyedrops than baseline IOP in the experimental eyes in the pilocarpine group,travoprost group and combination group,but no obvious change in IOP before and after use of eyedrops in the control eyes.There was no significant difference in the baseline IOP in both experimental eyes and control eyes,however,signifieant differences were seen in various time points after administration of eyedrops between experimental eyes and control eyes(P＜0.05).Compared with baseline IOP,IOP declined by 17.5％-22.0％ in pilocarpine group,23.8％-26.4％ travoprost group,27.6％-32.0％ in the combination group.For normal eye,piloearpine+travoprost showed a more power lowing IOP effect.Conclusions Hypotensive effect of combinative use of 2％ pilcoarpine and 0.004％ travoprost is strongest in comparison with individual use of pilocarpine or travoprost,but less than the statistical sum of individual use of these two drugs in a 24-day duration in normal eye of albino rabbit. Key words: Intraocular pressure; Prostaglandin analogus; Cholinomimetic drug; Pilocarpine; Travoprost

Effects of switching to SofZia-preserved travoprost in patients who presented with superficial punctate keratopathy while under treatment with latanoprost

To investigate the effects of switching to SofZia-preserved travoprost (TRV) on superficial punctate keratopathy (SPK) observed in patients using benzalkonium chloride (BAC)-preserved latanoprost (LAT). Patients with either primary open-angle glaucoma or ocular hypertension treated with LAT for at least 1 month who presented with SPK participated in this prospective, multicenter, open-label uncontrolled study. After the switch from LAT to TRV, patients were monitored at 2 weeks and at 1, 2, and 3 months. The use of concomitantly employed ophthalmic solutions was continued during the observation period. The intensity of SPK in each of five areas defined on the cornea was scored on a standard scale. Repeated measurements were tested with a linear mixed model. Of the 48 patients enrolled, 45 patients completed the study. After the switch to TRV, the mean SPK score in the whole cornea decreased significantly at every observation point (P < 0.0001 at each point) while intraocular pressure did not change significantly. Throughout the observation period, the SPK score tended to be higher in patients using a larger number of concomitant medications that contained BAC. Switching to TRV improved SPK observed in a population using LAT, likely because of a decrease in exposure to BAC.

Travoprost looks best for the budget in glaucoma

Travoprost looks best for the budget in glaucoma

Travoprost: profile report

Travoprost: profile report