Solid lipid nanoparticles for nose to brain delivery of donepezil: formulation, optimization by Box–Behnken design, <i>in vitro</i> and <i>in vivo</i> evaluation

Yasir, Mohd; Sara, Udai Vir Singh; Chauhan, Iti; Gaur, Praveen Kumar; Singh, Alok Pratap; Puri, Dinesh; Ameeduzzafar,

doi:10.1080/21691401.2017.1394872

Cited by 45 publications

(47 citation statements)

References 39 publications

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“…Al Asmari et al showed that liposomal formulation of donepezil with a size of 120 nm, significantly increased brain concentration after intranasal administration [12]. Similarly, pharmacokinetic and brain targeting studies in rats revealed a significantly high concentration of drug in brain following intranasal administration of solid lipid nanoparticles of donepezil in comparison with a donepezil solution [49]. This demonstrates brain targeting efficiency of solid lipid nanoparticles of 120 nm.…”

Section: Preparation Of Liposomesmentioning

confidence: 93%

Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

et al. 2020

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Direct nose-to-brain delivery has been raised as a non-invasive powerful strategy to deliver drugs to the brain bypassing the blood-brain barrier (BBB). This study aimed at preparing and characterizing an innovative composite formulation, associating the liposome and hydrogel approaches, suitable for intranasal administration. Thermosensitive gel formulations were obtained based on a mixture of two hydrophilic polymers (Poloxamer 407, P407 and Poloxamer 188, P188) for a controlled delivery through nasal route via liposomes of an active pharmaceutical ingredient (API) of potential interest for Alzheimer’s disease. The osmolarity and the gelation temperature (T° sol-gel) of formulations, defined in a ternary diagram, were investigated by rheometry and visual determination. Regarding the issue of assays, a mixture composed of P407/P188 (15/1%, w/w) was selected for intranasal administration in terms of T° sol-gel and for the compatibility with the olfactory mucosal (280 ± 20 mOsmol, pH 6). Liposomes of API were prepared by the thin film hydration method. Mucoadhesion studies were performed by using mucin disc, and they showed the good natural mucoadhesive characteristics of in situ gel formulations, which increased when liposomes were added. The study demonstrated successful pharmacotechnical development of a promising API-loaded liposomes in a thermosensitive hydrogel intended for nasal Alzheimer’s disease treatment.

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Section: Preparation Of Liposomesmentioning

confidence: 93%

Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

et al. 2020

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“…Such approach allowed obtaining different types of nanocarrier systems, ranging from nanostructured lipid carriers (NLC) to nanoemulsions. Tween® 80 was selected as the surfactant for the preparation of lipid nanoparticles because of its good emulsification efficacy and biocompatible nature for the solid lipid liquid mix [18,42]. Surfactant concentration was optimized envisioning the nanosystem stabilization, without compromising its colloidal and loading properties (i.e.…”

Section: Optimization Of the Lipid Nanoparticle Preparationmentioning

confidence: 99%

QbD-driven development of intranasal lipid nanoparticles for depression treatment

Vitorino

Silva

Gouveia

et al. 2020

European Journal of Pharmaceutics and Biopharmaceutics

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Depression is a life-threatening psychiatric disorder and a multifactorial global public health concern. Current pharmacological treatments present limited efficacy, and are associated with several harmful side effects and development of pharmacoresistance mechanisms. Developing more effective therapeutic options is therefore a priority. This work aims at efficiently designing an antidepressant therapeutic surrogate relying on a dual strategy supported on lipid nanoparticles and intranasal delivery. For that purpose, the formulation was comprehensively optimized following a quality by design perspective. Critical quality attributes (CQAs) ranged from physicochemical to intranasal performance features. The optimized formulation was administered to mice in order to assess the antidepressive and anxiolytic effects by applying the forced swimming and marble-burying tests, respectively. A cross-analysis of the predictive models established for the set of 12 CQAs elicited the formulation containing similar proportion of solid and liquid lipids and lower surfactant concentration as the optimal one. Despite increasing the liquid lipid amount yielded smaller and more homogeneous particle size, and higher release rate, nanostructured lipid carriers (NLCs) provided an earlier and superior pig nasal mucosa permeability than nanoemulsions, along with better stability and cytotoxic profiles. Importantly, the intranasal delivery of the optimal lipid nanoparticle formulation reduced both depressive and anxiety-like behaviors, which positions these intranasal nanosystems in line with the hypothesis of provisioning timely and better acting antidepressant therapies. 1. Introduction Depression is a life-threatening mental disorder and a major public health concern, affecting more than 300 million people of all ages worldwide [1]. It leads to disability, noteworthy health-related costs and decreased quality of life, being considered a prominent risk factor for many other diseases, including neuropsychiatric, cardiovascular, and metabolic conditions [2,3]. Conventional pharmacological treatments for depression are considered relatively well defined. Antidepressant standard-of-care comprises oral selective serotonin reuptake inhibitors (SSRIs, e.g. fluoxetine) and serotonin-norepinephrine reuptake inhibitors (SNRIs, e.g.

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“…Box-behnken design of the experiment was considered to be the best suitable design of the experiment for studying the effect of three variables at three levels. On applying the design of the experiment using design expert software total of 17 runs with 5 center points and 12 edge points within the design space were obtained [28]. All the 17 batches were prepared and their responses were recorded as shown in table 2.…”

Section: Preparation and Optimization By The Box-behnken Design Of Exmentioning

confidence: 99%

Preparation and Characterization of Etodolac Bearing Emulsomes

Gill

Nanda

2020

Int J App Pharm

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Objective: Emulsomes are novel vesicular drug delivery system with an internal solid lipid core surrounded by one or more bilayers of phospholipids. Etodolac is a potent anti-inflammatory drug and is a drug of choice for the treatment of various diseases. The present study is focused on the development of emulsomes using etodolac as drug candidates having improved drug loading with sustained-release effect for patient compliance. Methods: Emulsomes formulation composed of solid lipids (tristearin), phospholipids, cholesterol, stearylamine, and drug (etodolac) were prepared by lipid film hydration method followed by sonication to produce emulsomes of the nanometric size range. All the formulations were optimized by using box-behnken design of experiment considering 3 factors viz. drug to phospholipid ratio (A), tristearin to phospholipid ratio (B), stearylamine to phospholipid ratio (C) at 3 levels lower (-1), middle (0) and upper (+1). The response of the independent variables (A, B, C) was studied on the dependent variable viz. particle size (Y1), zeta potential (Y2), and entrapment efficiency (Y3). The responses were analyzed by design expert software to find out the optimized values of variables within the design space. Results: Compatibility with excipients was established by FTIR studies. The developed emulsomes were spherical shape vesicles as analyzed by TEM. The optimized batch (OB) was evaluated for particle size, zeta potential, and entrapment efficiency with experimental values 383.1 ± 11.7 nm, 47.2 ± 1.3 mV and 80.1 ± 3.2% and predicted values 390.394 nm, 45.000 mV and 81.642 %, respectively. The experimental values were found in reasonable agreement with predicted values by the design of the experiment. In vitro drug release study showed sustained release of the drug (88.69 % after 24 h). Conclusion: Etodolac loaded emulsomes is a novel drug delivery system and found to reliable in terms of various characteristic parameters like particle size, zeta potential, entrapment efficiency, and drug release. 3-factors 3-levels Box-behnken design of the experiment is a suitable design for the optimization of emulsomes.

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Solid lipid nanoparticles for nose to brain delivery of donepezil: formulation, optimization by Box–Behnken design, in vitro and in vivo evaluation

Cited by 45 publications

References 39 publications

Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

Pharmacotechnical Development of a Nasal Drug Delivery Composite Nanosystem Intended for Alzheimer’s Disease Treatment

QbD-driven development of intranasal lipid nanoparticles for depression treatment

Preparation and Characterization of Etodolac Bearing Emulsomes

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