ArticleAAPS PharmSciTech2009
Intranasal microemulsion of sildenafil citrate: in vitro evaluation and in vivo pharmacokinetic study in rabbits.
Article in AAPS PharmSciTech, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 99 citations in OpenAlex.
- Preparation,Pharmaceutical nanotechnology · 2025Article
- Nano-Emulsion Based Gel for Topical Delivery of an Anti-Inflammatory Drug: In vitro and in vivo Evaluation.Drug design, development and therapy · 2023Article
- Intranasal delivery of Clozapine using nanoemulsion-basedSaudi pharmaceutical journal : SPJ : the official publication of the Saudi Pharmaceutical Society · 2021Article
- Sildenafil 4.0-Integrated Synthetic Chemistry, Formulation and Analytical Strategies Effecting Immense Therapeutic and Societal Impact in the Fourth Industrial Era.Pharmaceuticals (Basel, Switzerland) · 2021Review
- Efficient Treatment of Experimental Cerebral Malaria by an Artemisone-SMEDDS System: Impact of Application Route and Dosing Frequency.Antimicrobial agents and chemotherapy · 2021Article
- Development of a Sildenafil Citrate Microemulsion-Loaded Hydrogel as a Potential System for Drug Delivery to the Penis and Its Cellular Metabolic Mechanism.Pharmaceutics · 2020Article
- Enhanced Bioavailability of Tadalafil after Intranasal Administration in Beagle Dogs.Pharmaceutics · 2018Article
- Preclinical Study of Ibuprofen Loaded Transnasal Mucoadhesive Microemulsion for Neuroprotective Effect in MPTP Mice Model.Iranian journal of pharmaceutical research : IJPR · 2018Article
- Article
- Optimized nano-transfersomal films for enhanced sildenafil citrate transdermal delivery: ex vivo and in vivo evaluation.Drug design, development and therapy · 2016Article
- Miconazole-loaded solid lipid nanoparticles: formulation and evaluation of a novel formula with high bioavailability and antifungal activity.International journal of nanomedicine · 2016Article
- Improvement of fluvastatin bioavailability by loading on nanostructured lipid carriers.International journal of nanomedicine · 2015Article
- Solid lipid nanoparticles loaded with iron to overcome barriers for treatment of iron deficiency anemia.Drug design, development and therapy · 2015Article
- Development of carbamazepine transnasal microemulsion for treatment of epilepsy.Drug delivery and translational research · 2013Article
- Comparative pharmacokinetic studies of borneol in mouse plasma and brain by different administrations.Journal of Zhejiang University. Science. B · 2012Article
- A nanohybrid system for taste masking of sildenafil.International journal of nanomedicine · 2012Article
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Authors and funding
3 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The purpose of the present study was to prepare intranasal delivery system of sildenafil citrate and estimate its relative bioavailability after nasal administration in rabbits to attain rapid onset of action with good efficacy at lower doses. Sildenafil citrate saturated solubility was determined in different solvents, cosolvents, and microemulsion systems. For nasal application, sildenafil citrate was formulated in two different systems: the first was a cosolvent system (S3) of benzyl alcohol/ethanol/water/Transcutol/taurodeoxy cholate/Tween 20 (0.5:16.8:47.7:15.9:1:18.1% w/w). The second was a microemulsion system (ME6) containing Oleic acid: Labrasol/Transcutol/water (8.33:33.3:16.66:41.66% w/w). The prepared systems were characterized in relation to their clarity, particle size, viscosity, pH, and nasal ciliotoxicity. In vivo pharmacokinetic performance of the selected system ME6 (with no nasal ciliotoxicity) was evaluated in a group of six rabbits in a randomized crossover study and compared to the marketed oral tablets. The targeted solubility (>20 mg/ml) of sildenafil citrate was achieved with cosolvent systems S1, S3, and S5 and with microemulsion systems ME3-ME6. The saturated solubility of sildenafil citrate in cosolvent system S3 and microemulsion system ME6 were 22.98 +/- 1.26 and 23.79 +/- 1.16 mg/ml, respectively. Microemulsion formulation ME6 showed shorter t (max) (0.75 h) and higher AUC((0-infinity)) (1,412.42 ng h/ml) compared to the oral tablets which showed t (max) equals 1.25 h and AUC((0-infinity)) of 1,251.14 ng h/ml after administration to rabbits at dose level of 5 mg/kg. The relative bioavailability was 112.89%. In conclusion, the nasal absorption of sildenafil citrate microemulsion was found to be fast, indicating the potential of nasal delivery instead of the conventional oral administration of such drug.
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Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.