Application of Statistical Tooling Techniques for Designing of Carvedilol Nanolipid Transferosomes and its Dermatopharmacokinetic and Pharmacodynamic Studies
| Autor: | Bhaskar Reddy Kesavan, Seshaiah K Sridhar, Brito R Selvaraj, Sucharitha Palagati |
|---|---|
| Rok vydání: | 2020 |
| Předmět: |
Male
Transdermal patch Drug Compounding Skin Absorption Adrenergic beta-Antagonists Biomedical Engineering Cmax Biological Availability Transdermal Patch Pharmaceutical Science Blood Pressure Permeability Dosage form Drug Delivery Systems Pharmacokinetics medicine Animals Particle Size Rats Wistar Carvedilol Transdermal Drug Carriers Models Statistical Chromatography Chemistry Transferosomes Nanostructures Rats Bioavailability Drug Liberation Kinetics Solubility Liposomes Models Animal medicine.drug |
| Zdroj: | Pharmaceutical Nanotechnology. 8:452-470 |
| ISSN: | 2211-7385 |
| DOI: | 10.2174/2211738508666200928164820 |
| Popis: | Background: The hypothesis is to augment the bioavailability and therapeutic potential of low bioavailable Carvedilol (25-35%) through Nanostructured Lipid Carrier (NLC) loaded Transdermal patch (Nanolipid Transferosomes). Methods: Box-Behnken design was designed to formulate NLC through a hot homogenization technique. About 17 formulations (C1-C17) were formulated by varying the critical material attribute and critical process parameter. Optimization was done based on its critical quality attributes like particle size, zeta potential and entrapment efficiency. Selected NLC (C16) has been fabricated into a transdermal patch through solvent evaporation technique and estimated for thickness, weight variation, moisture content, folding endurance, drug content, in vitro drug release, ex vivo skin permeation studies 48 hrs, in vitro drug release kinetic studies and skin irritation studies. In vivo pharmacokinetics and pharmacodynamic study parameters were compared between carvedilol loaded NLC transdermal patch and a conventional formulation (Coreg CR). Results: NLC (C16) was selected as the best formulation based on desirable, less particle size (201.1 ± 2.02 nm), more zeta potential (-37.2 ± 1.84mV) and maximum entrapment efficiency (87.54 ± 1.84%). Experimental investigations of in vivo dermatopharmacokinetic data shown statistically significant changes (p Conclusion: This research data concludes that NLC loaded transdermal patch (Nanolipid Transferosomes) was a suitable candidate to enhance the bioavailability of low bioavailable drug-like Carvedilol. Lay Summary: It was inferred from the literature that NLC filled transdermal patches were a novel strategy to increase the solubility and permeability of Carvedilol, which has less bioavailability. It reveals that there was no reproducible preparation for the NLC. It also reveals that the option of formulation and process parameters for the formation of NLC is not clearly justified. On account of this, an uniquely validated and optimized formulation technique was developed for NLC with low soluble and poorly bioavailable carvedilol, tested in Albino wistar rats for enhancement of bioavailability, the same study has been performed and proved. |
| Databáze: | OpenAIRE |
| Externí odkaz: |
|