Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances

Bertoni, Serena; Albertini, Beatrice; Passerini, Nadia

doi:10.3390/pharmaceutics12060548

Cited by 26 publications

(16 citation statements)

References 50 publications

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“…In fact, these values varied from 91.0% to 98.3% for the various formulations and the mean value was 95.5 ± 2.6%. Such a value is considerably higher compared to solvent-based emulsion methods and similar to those obtained with spray congealing process using one-phase materials [22,43,44].…”

Section: Drug Release From B-mpssupporting

confidence: 74%

Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure

et al. 2021

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Lipid-based biphasic microparticles are generally produced by long and complex techniques based on double emulsions. In this study, spray congealing was used as a solvent-free fabrication method with improved processability to transform water-in-oil non-aqueous emulsions into spherical solid lipid-based particles with a biphasic structure (b-MPs). Emulsions were prepared by melt emulsification using different compositions of lipids (Dynasan®118 and Compritol®888 ATO), surfactants (Cetylstearyl alcohol and Span®60) and hydrophilic carriers (PEGs, Gelucire®48/16 and Poloxamer 188). First, pseudo-ternary phase diagrams were constructed to identify the area corresponding to each emulsion type (coarse emulsion or microemulsion). The hydrophobicity of the lipid mostly affected the interfacial tension, and thus the microstructure of the emulsion. Emulsions were then processed by spray congealing and the obtained b-MPs were characterized in terms of thermal and chemical properties (by DSC and FT-IR), external and internal morphology (by SEM, CLSM and Raman mapping). Solid free-flowing spherical particles (main size range 200–355 µm) with different architectures were successfully produced: microemulsions led to the formation of particles with a homogeneous internal structure, while coarse emulsions generated “multicores-shell” particles consisting of variable size hydrophilic cores evenly distributed within the crystalline lipid phase. Depending on their composition and structure, b-MPs could achieve various release profiles, representing a more versatile system than microparticles based on a single lipid phase. The formulation and technological strategy proposed, provides a feasible and cost-effective way of fabricating b-MPs with tunable internal structure and release behavior.

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Section: Drug Release From B-mpssupporting

confidence: 74%

Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure

et al. 2021

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“…For the preparation, two solid lipids were chosen for which the ability to improve the bioavailability of poorly soluble active ingredients has been demonstrated in the literature [30]. The chosen lipids, Softisan 100, Capryol 90, and Gelucire 44/14, were conceived by evaluating the literature of recent years.…”

Section: Resultsmentioning

confidence: 99%

Optimization of Lipid Nanoparticles by Response Surface Methodology to Improve the Ocular Delivery of Diosmin: Characterization and In-Vitro Anti-Inflammatory Assessment

et al. 2022

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Diosmin is a flavonoid with a great variety of biological activities including antioxidant and anti-inflammatory ones. Its cytoprotective effect in retinal pigment epithelium cells under high glucose conditions makes it a potential support in the treatment of diabetic retinopathy. Despite its benefits, poor solubility in water reduces its potential for therapeutic use, making it the biggest biopharmaceutical challenge. The design of diosmin-loaded nanocarriers for topical ophthalmic application represents a novelty that has not been yet explored. For this purpose, the response surface methodology (RSM) was used to optimize nanostructured lipid carriers (NLCs), compatible for ocular administration, to encapsulate diosmin and improve its physicochemical issues. NLCs were prepared by a simple and scalable technique: a melt emulsification method followed by ultrasonication. The experimental design was composed of four independent variables (solid lipid concentration, liquid lipid concentration, surfactant concentration and type of solid lipid). The effect of the factors was assessed on NLC size and PDI (responses) by analysis of variance (ANOVA). The optimized formulation was selected according to the desirability function (0.993). Diosmin at two different concentrations (80 and 160 µM) was encapsulated into NLCs. Drug-loaded nanocarriers (D-NLCs) were subjected to a physicochemical and technological investigation revealing a mean particle size of 83.58 ± 0.77 nm and 82.21 ± 1.12 nm, respectively for the D-NLC formulation prepared with diosmin at the concentration of 80 µM or 160 µM, and a net negative surface charge (−18.5 ± 0.60 and −18.0 ± 1.18, respectively for the two batches). The formulations were analyzed in terms of pH (6.5), viscosity, and adjusted for osmolarity, making them more compatible with the ocular environment. Subsequently, stability studies were carried out to assess D-NLC behavior under different storage conditions up to 60 days, indicating a good stability of NLC samples at room temperature. In vitro studies on ARPE-19 cells confirmed the cytocompatibility of NLCs with retinal epithelium. The effect of D-NLCs was also evaluated in vitro on a model of retinal inflammation, demonstrating the cytoprotective effect of D-NLCs at various concentrations. RSM was found to be a reliable model to optimize NLCs for diosmin encapsulation.

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“…In this technique, the drug is dissolved/dispersed in polymeric solution, that is, lipophilic polymer like wax. The hot molten solution then sprayed to form fine droplets into a vessel that already kept in carbon dioxide ice bath [45].…”

Section: Spray Congealingmentioning

confidence: 99%

A Review on Microspheres as a Novel Controlled Drug Delivery System

Samanta¹,

Gautam²,

Chandel³

et al. 2021

Asian J Pharm Clin Res

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Over the past three decades, controlled drug delivery systems have become more developed and play a key role in pharmaceuticals formulations. There are many shortcomings in Traditional or Conventional drug delivery systems like for maintaining desired therapeutic drug plasma concentration there is a need for frequent dosing for particular drugs having shorter half-lives. Furthermore, because of frequent dosing requirement, there is poor patient compliance which causes fluctuation in plasma concentration of the drug. The limitations of conventional drug delivery can be overcome by the development of novel drug delivery systems, of which the controlled drug delivery can maintain constant drug plasma concentration by slowly releasing the drug over an extended period. Developing controlled drug delivery systems can also improve the systemic bioavailability of the drug, thus enhancing the therapeutic efficacy of the drug and better patient compliance. There are many different approaches for such controlled delivery systems such as liposomes, niosomes, ethosomes, phytosomes, microemulsion, and microspheres. Among all the approaches microspheres are more convenient as the drug is slowly released from the polymeric matrix and the polymers used are mostly biodegradable and possess no side effects. Therefore, microspheres can be used in various medicinal departments such as oncology, gynecology, radiology, pulmonary, cardiology, diabetes, and vaccine therapy. This review article focuses on recent different types of microspheres along with their methods of preparation. The microspheres formulated can be later evaluated and characterized by different procedures.

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Different BCS Class II Drug-Gelucire Solid Dispersions Prepared by Spray Congealing: Evaluation of Solid State Properties and In Vitro Performances

Cited by 26 publications

References 50 publications

Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure

Solvent-Free Fabrication of Biphasic Lipid-Based Microparticles with Tunable Structure

Optimization of Lipid Nanoparticles by Response Surface Methodology to Improve the Ocular Delivery of Diosmin: Characterization and In-Vitro Anti-Inflammatory Assessment

A Review on Microspheres as a Novel Controlled Drug Delivery System

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