Approach to tune drug release in particles fabricated from methacrylate functionalized polylactides

2021 ◽  
Author(s):  
Boris Shavkuta ◽  
Kseniia Bardakova ◽  
Yana Khristidis ◽  
Nikita V. Minaev ◽  
Anastasia Frolova ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Surface Topography ◽  
Degradation Rate ◽  
Drug Loading

Different particles' mechanical properties and surface topography that significantly influenced the degradation rate, drug loading, and release.

scholarly journals Artificial, Triple-Layered, Nanomembranous Wound Patch for Potential Diabetic Foot Ulcer Intervention

Materials ◽  
2018 ◽  
Vol 11 (11) ◽  
pp. 2128 ◽  
Author(s):  
Mostafa Mabrouk ◽  
Pradeep Kumar ◽  
Yahya E. Choonara ◽  
Lisa C. du Toit ◽  
Viness Pillay
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Diabetic Foot ◽  
Drug Loading ◽  
Foot Ulcer ◽  
Diabetic Foot Ulcer ◽  
Middle Layer ◽  
Patch Quality ◽  
Moisture Uptake

The present work aims to electrospin a triple layered wound patch for potential treatment of diabetic foot ulcers (DFU). The patch consisted of poly(acrylic acid) (PAA) as the skin contacting layer, polyvinyl pyrrolidone (PVP) as the middle layer, and polycaprolactone (PCL) as the outermost layer, wherein the PVP layer was loaded in situ with an antibiotic (ciprofloxacin, CFX). Morphology and mechanical properties were investigated using SEM and texture analysis. Patch quality was studied with regards to wettability, adherence, water resistance, and moisture uptake of individual layers. SEM results confirmed the fibrous and membranous nature of layers with a nano-to-micro size range. Mechanical properties of the composite patch demonstrated a tensile strength of 12.8 ± 0.5 MPa, deformation energy of 54.35 ± 0.1 J/m3, and resilience of 17.8 ± 0.7%, which were superior compared to individual layers. Patch quality tests revealed that the PCL layer showed very low wettability, adherence, and moisture uptake compared to the PVP and PAA layers. In vitro drug release data revealed an increase in cumulative drug release with higher drug loading. The results above confirm the potential of a triple layered, tripolymeric, wound patch for DFU intervention.

scholarly journals INVESTIGATION ON THE MECHANICAL, THERMAL, BIO-DEGRADATION, AND BIO-COMPATIBILITY PROPERTIES OF POLY (LACTIC ACID) / POLY (ETHYLENE GLYCOL) BLEND

2021 ◽  
Vol 22 (1) ◽  
pp. 223-233
Author(s):  
Zohreh Zarinkolah ◽  
Hamed Bagheri ◽  
Saman Hosseinkhani ◽  
Maryam Nikkhah
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Drug Loading ◽  
Poly Lactic Acid ◽  
Burst Release ◽  
Mechanical And Thermal Properties ◽  
Cytotoxicity Test ◽  
Test Results ◽  
Drug Release Profile ◽  
Absorbable Sutures

Absorbable sutures are widely used in surgery. In addition to acceptable mechanical properties, the surgical sutures should exhibit favorable degradability properties. In this research, the mechanical and thermal properties, hydrophilicity, biodegradability, pH changes, and drug release profile of polylactic acid (PLA) and polyethylene glycol (PEG) alloy were examined to fabricate absorbable sutures. The test results for the mechanical properties showed that the strength of the PLA/PEG alloy decreased with increasing PEG content, leading to an increase in elongation. The differential thermal analysis indicated that the resulting material was above its glass transition temperature (Tg) at ambient temperature and was thus flexible enough. According to the degradation test results, the alloys were degraded similar to the commercial sample. Furthermore, the pH measurements revealed that the degradation of the alloy had no significant effect on the pH of the environment. Bupivacaine hydrochloride was incorporated into a certain amount of PLA and PEG, and the drug release rate was then measured. The sample provided a suitable substrate for burst release. Moreover, the cytotoxicity test was carried out to evaluate the biocompatibility properties of the PLA/PEG alloy and it was found that this alloy is biocompatible and the biocompatibility of the material decreases with increasing drug loading. ABSTRAK: Sutur boleh serap telah digunakan dalam pembedahan secara meluas. Tambahan kepada sifat-sifat mekanikal ini, sutur pembedahan perlu memiliki ciri-ciri kebolehurain yang dikehendaki. Dalam kajian ini, sifat-sifat mekanikal dan terma, kehidrofilikan, kebolehuraian, perubahan pH, dan profil penguraian ubat asid polilaktik (PLA) dan aloi polietilena glikol (PEG) telah dikaji bagi mencipta sutur boleh serap. Hasil kajian mendapati sifat-sifat mekanikal menunjukkan kekuatan PLA/PEG aloi berkurangan dengan penambahan level PEG, menyebabkan bertambahnya pemanjangan. Analisis pembezaan terma menunjukkan hasil bahan adalah melepasi suhu perubahan gelas (Tg) pada suhu sekitar dan oleh itu sangat lentur. Berdasarkan hasil kajian degradasi, aloi ini telah digradasi seperti sampel komersial. Tambahan lagi, ukuran pH menunjukkan degradasi aloi ini tidak menunjukkan kesan langsung pada pH persekitaran. Bupivacaine hidroklorida dimasukkan ke dalam PLA dan PEG, dan kadar ubat dibebaskan kemudiannya diukur. Sampel substrat yang bersesuian disediakan bagi pelepas letus. Tambahan, ujian Kesitotoksikan telah dijalankan bagi menilai ciri-ciri keserasian-bio aloi PLA/PEG dan didapati aloi ini serasi-bio dan keserasian-bio bahan berkurangan dengan penambahan beban ubat.

DLP 3D printing of Dexamethasoneincorporated PEGDA-based photopolymers: compressive properties and drug release

2020 ◽  
Vol 6 (3) ◽  
pp. 406-409
Author(s):  
Robert Mau ◽  
Thomas Reske ◽  
Thomas Eickner ◽  
Niels Grabow ◽  
Hermann Seitz
Keyword(s):  
Mechanical Properties ◽  
3D Printing ◽  
Drug Release ◽  
Drug Loading ◽  
Patient Specific ◽  
Burst Release ◽  
Compressive Properties ◽  
Drug Load ◽  
Polyethylene Glycol Diacrylate ◽  
3D Printed

AbstractPhotopolymerizing, high-resolution 3D printing methods such as Stereolithography (SLA) or Digital Light Processing (DLP) are very promising for the manufacturing of drug-incorporated, patient specific implants. However, a drug-load may be limited by adequately solubility of the active pharmaceutical ingredient (API) in the photopolymer. Furthermore, a drug-load may affect the mechanical properties of the material negatively. Here, we investigate the DLP 3D printing of drugincorporated photopolymers. Polyethylene glycol diacrylate (PEGDA, Mn = 700 g/mol) is used as matrix polymer and Dexamethasone (DEX) is used for drug-loading (10 g/L and 20 g/L). Compressive properties, drug release and drug stability of 3D printed test samples were analyzed. DEX was found to be sparingly soluble in the PEGDA-based photopolymer. Not all drug particles can be dissolved at a concentration of 20 g/L and a slurry-like suspension is formed. Drug-incorporated photopolymers of 10 g/L (solution) and 20 g/L (suspension) were processed successfully via DLP. The higher the drug-load, the lower the compressive strength. Mechanical properties can be improved via a post-curing in a UV light curing box. Drug-incorporated 3D printed test samples show burst-release of DEX. The post-curing process does not affect drug release. DEX degrades in 3D-printed test samples significantly (~ 30 %) over a several days time period.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Formulating SLN and NLC as Innovative Drug Delivery Systems for Non-Invasive Routes of Drug Administration

2020 ◽  
Vol 27 (22) ◽  
pp. 3623-3656 ◽  
Author(s):  
Bruno Fonseca-Santos ◽  
Patrícia Bento Silva ◽  
Roberta Balansin Rigon ◽  
Mariana Rillo Sato ◽  
Marlus Chorilli
Keyword(s):  
Drug Delivery ◽  
Particle Size ◽  
Drug Release ◽  
Drug Loading ◽  
Average Particle Size ◽  
Delivery Systems ◽  
Average Particle ◽  
Minor Importance ◽  
Routes Of Administration ◽  
Non Invasive

Colloidal carriers diverge depending on their composition, ability to incorporate drugs and applicability, but the common feature is the small average particle size. Among the carriers with the potential nanostructured drug delivery application there are SLN and NLC. These nanostructured systems consist of complex lipids and highly purified mixtures of glycerides having varying particle size. Also, these systems have shown physical stability, protection capacity of unstable drugs, release control ability, excellent tolerability, possibility of vectorization, and no reported production problems related to large-scale. Several production procedures can be applied to achieve high association efficiency between the bioactive and the carrier, depending on the physicochemical properties of both, as well as on the production procedure applied. The whole set of unique advantages such as enhanced drug loading capacity, prevention of drug expulsion, leads to more flexibility for modulation of drug release and makes Lipid-based nanocarriers (LNCs) versatile delivery system for various routes of administration. The route of administration has a significant impact on the therapeutic outcome of a drug. Thus, the non-invasive routes, which were of minor importance as parts of drug delivery in the past, have assumed added importance drugs, proteins, peptides and biopharmaceuticals drug delivery and these include nasal, buccal, vaginal and transdermal routes. The objective of this paper is to present the state of the art concerning the application of the lipid nanocarriers designated for non-invasive routes of administration. In this manner, this review presents an innovative technological platform to develop nanostructured delivery systems with great versatility of application in non-invasive routes of administration and targeting drug release.

Mesoporous Silica Molecular Sieve based Nanocarriers: Transpiring Drug Dissolution Research

2017 ◽  
Vol 23 (3) ◽  
pp. 467-480 ◽  
Author(s):  
Satyanarayan Pattnaik ◽  
Kamla Pathak
Keyword(s):  
Drug Release ◽  
Mesoporous Silica ◽  
Molecular Sieves ◽  
Release Kinetics ◽  
Drug Loading ◽  
Scale Up ◽  
Water Soluble ◽  
Drug Dissolution ◽  
Water Soluble Drugs ◽  
Loading Methods

Background: Improvement of oral bioavailability through enhancement of dissolution for poorly soluble drugs has been a very promising approach. Recently, mesoporous silica based molecular sieves have demonstrated excellent properties to enhance the dissolution velocity of poorly water-soluble drugs. Description: Current research in this area is focused on investigating the factors influencing the drug release from these carriers, the kinetics of drug release and manufacturing approaches to scale-up production for commercial manufacture. Conclusion: This comprehensive review provides an overview of different methods adopted for synthesis of mesoporous materials, influence of processing factors on properties of these materials and drug loading methods. The drug release kinetics from mesoporous silica systems, the manufacturability and stability of these formulations are reviewed. Finally, the safety and biocompatibility issues related to these silica based materials are discussed.

scholarly journals Novel Hydrogels of Chitosan and Poly (vinyl alcohol) Reinforced with Inorganic Particles of Bioactive Glass

Polymers ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 691
Author(s):  
O. Sánchez-Aguinagalde ◽  
Ainhoa Lejardi ◽  
Emilio Meaurio ◽  
Rebeca Hernández ◽  
Carmen Mijangos ◽  
...  
Keyword(s):  
Mechanical Properties ◽  
Drug Release ◽  
Bioactive Glass ◽  
Vinyl Alcohol ◽  
Release Kinetics ◽  
The Body ◽  
Poly Vinyl Alcohol ◽  
X Ray Diffraction ◽  
Inorganic Particles ◽  
Release Studies

Chitosan (CS) and poly (vinyl alcohol) (PVA) hydrogels, a polymeric system that shows a broad potential in biomedical applications, were developed. Despite the advantages they present, their mechanical properties are insufficient to support the loads that appear on the body. Thus, it was proposed to reinforce these gels with inorganic glass particles (BG) in order to improve mechanical properties and bioactivity and to see how this reinforcement affects levofloxacin drug release kinetics. Scanning electron microscopy (SEM), X-ray diffraction (XRD), swelling tests, rheology and drug release studies characterized the resulting hydrogels. The experimental results verified the bioactivity of these gels, showed an improvement of the mechanical properties and proved that the added bioactive glass does affect the release kinetics.

Preparation, evaluation, and in vitro release of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules

2020 ◽  
pp. 1-9
Author(s):  
Yunhong Wang ◽  
Rong Hu ◽  
Yanlei Guo ◽  
Weihan Qin ◽  
Xiaomei Zhang ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Rate ◽  
Orthogonal Design ◽  
Drug Loading ◽  
In Vitro Release ◽  
Core Material ◽  
Evaluation Indexes ◽  
Vitro Release

OBJECTIVE: In this study we explore the method to prepare tanshinone self-microemulsifying sustained-release microcapsules using tanshinone self-microemulsion as the core material, and chitosan and alginate as capsule materials. METHODS: The optimal preparation technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules was determined by using the orthogonal design experiment and single-factor analysis. The drug loading and entrapment rate were used as evaluation indexes to assess the quality of the drug, and the in vitro release rate was used to evaluate the drug release performance. RESULTS: The best technology of chitosan-alginate tanshinone self-microemulsifying sustained-release microcapsules is as follows: the concentration of alginate is 1.5%, the ratio of tanshinone self-microemulsion volume to alginate volume to chitosan mass is 1:1:0.5 (ml: ml: g), and the best concentration of calcium chloride is 2.0%. To prepare the microcapsules using this technology, the drug loading will be 0.046%, the entrapment rate will be 80.23%, and the 24-hour in vitro cumulative release rate will be 97.4%. CONCLUSION: The release of the microcapsules conforms to the Higuchi equation and the first-order drug release model and has a good sustained-release performance.

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