Novel surface modified solid lipid nanoparticles as intranasal carriers for ropinirole hydrochloride: application of factorial design approach
Open accessAbstract
Present investigation deals with intranasal delivery of ropinirole hydrochloride (ROPI HCl), loaded in solid lipid nanoparticles (SLNs). Prime objectives of this experiment are avoidance of hepatic first pass metabolism and to improve therapeutic efficacy in the treatment of Parkinson's disease. SLNs were fabricated by emulsification-solvent diffusion technique. A 3(2)-factorial design approach has been employed to assess the influence of two independent variables, namely Pluronic F-68 and stearylamine concentration on particle size, ζ-potential and entrapment efficiency of prepared SLNs. Prepared samples were further evaluated for in vitro drug diffusion, ex vivo drug permeation, histopathological and stability studies. Differential scanning calorimetry analysis revealed the encapsulation of amorphous form of drug into lipid matrix, while scanning electron microscopy studies indicated the spherical shape. Fabricated SLNs had shown no severe signs of damage on integrity of nasal mucosa. Release pattern of prepared drug-loaded sample was best fitted to zero-order kinetic model with non-Fickian super case II diffusion mechanism. In vivo pharmacodynamic studies were carried out to compare therapeutic efficacy of prepared nasal formulation against marketed oral formulation. Results of analysis of variance demonstrated the significance of suggested model. Three-dimensional response surface plots and regression equations confirmed the corresponding influence of selected independent variables on measured responses. Our findings suggested the feasibility of investigated system for intranasal administration.
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Sustained delivery and higher bioavailability of ropirinole, bromocriptine and apomorphine could be achieved through SLNs.
“Sustained delivery and higher bioavailability of ropirinole, bromocriptine and apomorphine could be achieved through SLNs.126,127”
From Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles (2019) · cites this paper as [126]
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Targeted therapy in chronic diseases using nanomaterial-based drug delivery vehicles
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- Authors
- Pardeshi, C. V., Rajput, P. V., Belgamwar, V. S., Tekade, A. R., & Surana, S. J.
- Corresponding author
- Tekade, Avinash R.
- Venue
- Drug Delivery
- Publisher
- Informa UK Limited
- Published
- 2013-01
- Volume
- 20
- Issue
- 1
- Pages
- 47-56
- ISSN
- 1071-7544 (ISSN-L)
- 1521-0464
- OpenAlex
- W2148465626
- Cited by
- 141
- References
- 29
- Citations by year
- 2026: 10 · 2025: 9 · 2024: 12 · 2023: 17 · 2022: 17 · 2021: 20 · 2020: 11 · 2019: 11 · 2018: 8 · 2017: 4 · 2016: 9 · 2015: 9 · 2014: 2 · 2013: 2
- FWCI
- 4.42
- Type
- journal article
- Language
- en
- Open access
- bronze
- doi.org
- Locations
- Drug Delivery (publishedVersion)
- PubMed (publishedVersion)
- Topics
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advanced Drug Delivery Systems
- Life Sciences › Pharmacology, Toxicology and Pharmaceutics › Pharmaceutical Science › Advancements in Transdermal Drug Delivery
- Health Sciences › Medicine › Pulmonary and Respiratory Medicine › Inhalation and Respiratory Drug Delivery
- Keywords
- solid lipid nanoparticles, ropinirole hydrochloride, intranasal drug delivery, Parkinson's disease, surface modification, poloxamer 188, octadecylamine, factorial design, particle size, zeta potential, encapsulation efficiency, nasal mucosa, drug release kinetics, first-pass metabolism avoidance
- MeSH terms
- Administration, Intranasal, Animals, Antiparkinson Agents, Drug Carriers, Indoles, Lipids, Male, Nasal Mucosa, Organ Culture Techniques, Sheep, Surface Properties, Mice, Nanoparticles
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