Development and validation of an in vitro release method for topical particulate delivery systems

Kregar, Maja Lusina; Dürrigl, Marjana; Rožman, Andrea; Jelčić, Želimir; Cetina-Čižmek, Biserka; Filipović-Grčić, Jelena

doi:10.1016/j.ijpharm.2015.03.018

Cited by 20 publications

(4 citation statements)

References 29 publications

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“…One of the most important steps in the study of the efficacy of new delivery systems is the in vitro drug release analysis. Topical carriers are an advanced form of powders for which, so far, there are no compendial or standard release techniques and apparatuses [31,32]. Therefore, several in vitro drug release methods have been used: for example, dialysis [8,12,31,69], Franz cells [23,31,40,70], paddle or basket apparatuses [11,71], flow through cells [8,40].…”

Section: Resultsmentioning

confidence: 99%

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Formulation and Characterization of Native and Crosslinked Hyaluronic Acid Microspheres for Dermal Delivery of Sodium Ascorbyl Phosphate: A Comparative Study

et al. 2018

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The present work evaluates for the first time the use of urea-crosslinked hyaluronic acid (HA-CL), a novel derivative of native hyaluronic acid (HA), to produce microspheres (MS) by emulsification-solvent evaporation, for dermal delivery of sodium ascorbyl phosphate (SAP). As the term of comparison, HA MS were prepared. A pre-formulation study—investigation of the effects of polymers solutions properties (pH, viscosity) and working conditions—led to the production of optimized HA-CL MS and HA-CL—SAP MS with: almost unimodal size distributions; mean diameter of 13.0 ± 0.7 and 9.9 ± 0.8 µm, respectively; spherical shape and rough surface; high yield, similar to HA MS and HA–SAP MS (≈ 85%). SAP was more efficiently encapsulated into HA-CL MS (78.8 ± 2.6%) compared to HA MS (69.7 ± 4.6%). Physical state, thermal properties, relative moisture stability of HA-CL MS and HA-CL–SAP MS were comparable to those of HA MS and HA–SAP MS. However, HA-CL–SAP MS exhibited an extended drug release compared to HA–SAP MS, despite the same kinetic mechanism—contemporaneous drug diffusion and polymer swelling/dissolution. Therefore, HA-CL formulation showed a greater potential as microcarrier (for encapsulation efficiency and release kinetic), that could be improved, in future, using suitable excipients.

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Section: Resultsmentioning

confidence: 99%

“…For topical microcarriers, there are no compendial or standard release methods and apparatuses [31,32]. Therefore, in vitro release profiles of SAP from HA and HA-CL MS were evaluated with two different methodologies, under different experimental conditions.…”

Section: Methodsmentioning

confidence: 99%

Formulation and Characterization of Native and Crosslinked Hyaluronic Acid Microspheres for Dermal Delivery of Sodium Ascorbyl Phosphate: A Comparative Study

et al. 2018

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“…The in vitro release experiments were performed according to the method developed by Lusina Kregar et al, 2015 [28], with slight modifications. A VK7010 dissolution apparatus with 200 mL flat-bottom vessels and mini-paddles (Agilent Technologies) was used.…”

Section: In Vitro Release Testing Of Van-loaded Plga Microparticlesmentioning

confidence: 99%

Selection of Excipients for the Preparation of Vancomycin-Loaded Poly(D,L-lactide-co-glycolide) Microparticles with Extended Release by Emulsion Spray Drying

Jurić Simčić,

Erak,

Cetina Čižmek

et al. 2023

Pharmaceutics

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The aim of this study was to relate the composition of the W/O emulsion used as a starting fluid in the spray-drying process to the quality of the dry polymer particles obtained in terms of physical–chemical properties, compatibility and drug release performance. Four W/O emulsions containing vancomycin hydrochloride (VAN), an encapsulating PLGA polymer and Poloxamer® 407, chitosan and/or sorbitan monooleate as stabilisers were spray-dried using an ultrasonic atomising nozzle. The microparticles obtained were micron-sized, with a volume mean diameter between 43.2 ± 0.3 and 64.0 ± 12.6 µm, and spherical with a mostly smooth, non-porous surface and with high drug loading (between 14.5 ± 0.6 and 17.1 ± 1.9% w/w). All formulations showed a prolonged and biphasic VAN release profile, with diffusion being the primary release mechanism. Microparticles prepared from the emulsions with Poloxamer® 407 and sorbitan monooleate released VAN rapidly and completely within one day. The release of VAN from microparticles prepared from the emulsion without additives or with chitosan in the inner aqueous phase was significantly decreased; after four days, a cumulative release of 65% and 61%, respectively, was achieved. Microparticles with encapsulated chitosan had the largest mean particle diameter and the slowest release of VAN.

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“…The following requirements were considered: relative standard deviation (RSD) of the detector response and retention time for all standard injections was not more than 2%, capacity factor (k') was higher than 2, tailing factor (T) of drug peak was not more than 2.0, and theoretical plate number (N) was higher than 2000. These parameters were obtained by injecting five times an intermediate standard for each drug [22].…”

Section: System Suitabilitymentioning

confidence: 99%

Fast Screening Methods for the Analysis of Topical Drug Products

Miranda

Cardoso²,

Vitorino

2020

Processes

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Considering the recent regulatory requirements, the overall importance of in vitro release testing (IVRT) methods regarding topical product development is undeniable, especially when addressing particulate systems. For each IVRT study, several hundreds of samples are generated. Therefore, developing rapid reversed-phase high-performance liquid chromatography (RP-HPLC) methods, able to provide a real-time drug analysis of IVRT samples, is a priority. In this study, eight topical complex drug products exhibiting distinct physicochemical profiles were considered. RP-HPLC methods were developed and fully validated. Chromatographic separations were achieved on a XBridgeTM C18 (5 µm particle size, 150 mm × 2.1 mm), or alternatively on a LiChrospher® 100 RP-18 (5 µm particle size, 125 mm × 4.6 mm) at 30 °C, under isocratic conditions using UV detection at specific wavelengths. According to the physicochemical characteristics of each drug, different mobile phases were selected. Irrespective of the drug (hydrocortisone, etofenamate, bifonazole, clotrimazole, acyclovir, tioconazole, clobetasol, and diclofenac) and formulation, retention time values did not exceed 6.5 min. All methods were linear, specific, precise, and accurate at the intraday and interday levels, robust, and stable. These were successfully applied to establish product-specific IVRT profiles, thus providing a key database useful for topical pharmaceutical manufacturers.

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Development and validation of an in vitro release method for topical particulate delivery systems

Cited by 20 publications

References 29 publications

Formulation and Characterization of Native and Crosslinked Hyaluronic Acid Microspheres for Dermal Delivery of Sodium Ascorbyl Phosphate: A Comparative Study

Formulation and Characterization of Native and Crosslinked Hyaluronic Acid Microspheres for Dermal Delivery of Sodium Ascorbyl Phosphate: A Comparative Study

Selection of Excipients for the Preparation of Vancomycin-Loaded Poly(D,L-lactide-co-glycolide) Microparticles with Extended Release by Emulsion Spray Drying

Fast Screening Methods for the Analysis of Topical Drug Products

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