A Novel Hollow Hydroxyapatite Microspheres/Chitosan Composite Drug Carrier for Controlled Release

Background: Using imatinib, a tyrosine kinase inhibitor drug used in lymphoblastic leukemia, has always had limitations due to its cardiotoxicity and hepatotoxicity side effects. The objective of this study is to develop a target-oriented drug carrier to minimize these adverse effects by the controlled release of the drug. Methods: KIT-5 nanoparticles were functionalized with 3-aminopropyltriethoxysilane and conjugated to rituximab as the targeting agent for the CD20 positive receptors of the B-cells. Then they were loaded with imatinib and their physical properties were characterized. The cell cytotoxicity of the nanoparticles was studied by MTT assay in Ramos (CD20 positive) and Jurkat cell lines (CD20 negative) and their cellular uptake was shown by fluorescence microscope. Wistar rats received an intraperitoneal injection of 50 mg/kg of the free drug or targeted nanoparticles for 21 days. Then the level of aspartate Aminotransferase (AST), alanine Aminotransferase (ALT), Alkaline Phosphatase (ALP) and Lactate Dehydrogenase (LDH) were measured in serum of animals. The cardiotoxicity and hepatotoxicity of the drug were also studied by hematoxylin and eosin staining of the tissues. Results: The targeted nanoparticles of imatinib showed to be more cytotoxic to Ramos cells rather than Jurkat cells. The results of the biochemical analysis displayed a significant reduction in AST, ALT, ALP, and LDH levels in animals treated with targeted nanoparticles, compared to the free drug group. By comparison with the free imatinib, histopathological results represented less cardiotoxicity and hepatotoxicity in the animals, which received the drug through the current designed delivery system. Conclusion: The obtained results confirmed that the rituximab targeted KIT-5 nanoparticles are promising in the controlled release of imatinib and could decrease its cardiotoxicity and hepatotoxicity side effects.

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Formulation and development of metformin-loaded microspheres using Khaya senegalensis (Meliaceae) gum as co-polymer

Future Journal of Pharmaceutical Sciences ◽

10.1186/s43094-020-00139-6 ◽

2020 ◽

Vol 6 (1) ◽

Author(s):

Chukwuebuka H. Ozoude ◽

Chukwuemeka P. Azubuike ◽

Modupe O. Ologunagba ◽

Sejoro S. Tonuewa ◽

Cecilia I. Igwilo

Keyword(s):

Controlled Release ◽

Sodium Alginate ◽

Release Kinetics ◽

Drug Carrier ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Metformin Hydrochloride ◽

Scanning Calorimetry ◽

Khaya Senegalensis

Abstract Background Khaya gum is a bark exudate from Khaya senegalensis (Maliaecae) that has drug carrier potential. This study aimed to formulate and comparatively evaluate metformin-loaded microspheres using blends of khaya gum and sodium alginate. Khaya gum was extracted and subjected to preformulation studies using established protocols while three formulations (FA; FB and FC) of metformin (1% w/v)-loaded microspheres were prepared by the ionic gelation method using 5% zinc chloride solution as the cross-linker. The formulations contained 2% w/v blends of khaya gum and sodium alginate in the ratios of 2:3, 9:11, and 1:1, respectively. The microspheres were evaluated by scanning electron microscopy, Fourier transform-infrared spectroscopy, differential scanning calorimetry, entrapment efficiency, swelling index, and in vitro release studies. Results Yield of 28.48%, pH of 4.00 ± 0.05, moisture content (14.59% ± 0.50), and fair flow properties (Carr’s index 23.68 ± 1.91 and Hausner’s ratio 1.31 ± 0.03) of the khaya gum were obtained. FTIR analyses showed no significant interaction between pure metformin hydrochloride with excipients. Discrete spherical microspheres with sizes ranging from 1200 to 1420 μm were obtained. Drug entrapment efficiency of the microspheres ranged from 65.6 to 81.5%. The release of the drug from microspheres was sustained for the 9 h of the study as the cumulative release was 62% (FA), 73% (FB), and 80% (FC). The release kinetics followed Korsmeyer-Peppas model with super case-II transport mechanism. Conclusion Blends of Khaya senegalensis gum and sodium alginate are promising polymer combination for the preparation of controlled-release formulations. The blend of the khaya gum and sodium alginate produced microspheres with controlled release properties. However, the formulation containing 2:3 ratio of khaya gum and sodium alginate respectively produced microspheres with comparable controlled release profiles to the commercial brand metformin tablet.

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Hydrogel Nanofibers from Carboxymethyl Sago Pulp and Its Controlled Release Studies as a Methylene Blue Drug Carrier

Fibers ◽

10.3390/fib7060056 ◽

2019 ◽

Vol 7 (6) ◽

pp. 56 ◽

Cited By ~ 3

Author(s):

Nafeesa Mohd Kanafi ◽

Norizah Abdul Rahman ◽

Nurul Husna Rosdi ◽

Hasliza Bahruji ◽

Hasmerya Maarof

Keyword(s):

Methylene Blue ◽

Citric Acid ◽

Controlled Release ◽

Drug Carrier ◽

Curing Temperature ◽

Buffer Solution ◽

Release Studies ◽

Electrospinning Method ◽

Poly Ethylene Oxide ◽

Poly Ethylene

The potential use of carboxymethyl sago pulp (CMSP) extracted from sago waste for producing hydrogel nanofibers was investigated as a methylene blue drug carrier. Sago pulp was chemically modified via carboxymethylation reaction to form carboxymethyl sago pulp (CMSP) and subsequently used to produce nanofibers using the electrospinning method with the addition of poly(ethylene oxide) (PEO). The CMSP nanofibers were further treated with citric acid to form cross-linked hydrogel. Studies on the percentage of swelling following the variation of citric acid concentrations and curing temperature showed that 89.20 ± 0.42% of methylene blue (MB) was loaded onto CMSP hydrogel nanofibers with the percentage of swelling 4366 ± 975%. Meanwhile, methylene blue controlled release studies revealed that the diffusion of methylene blue was influenced by the pH of buffer solution with 19.44% of MB released at pH 7.34 within 48 h indicating the potential of CMSP hydrogel nanofibers to be used as a drug carrier for MB.

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Transport Properties for Pharmaceutical Controlled-Release Systems: A Brief Review of the Importance of Their Study in Biological Systems

Biomolecules ◽

10.3390/biom8040178 ◽

2018 ◽

Vol 8 (4) ◽

pp. 178 ◽

Cited By ~ 4

Author(s):

Ana C. F. Ribeiro ◽

Miguel A. Esteso

Keyword(s):

Controlled Release ◽

Transport Properties ◽

Diffusion Coefficients ◽

Drug Carrier ◽

Strong Association ◽

Mutual Diffusion ◽

Mixed Electrolytes ◽

Coupled Transport ◽

Concentration Gradients ◽

Enhanced Solubility

: The goal of this work was to comprehensive study the transport properties of controlled-release systems for the safe and reliable delivery of drugs. Special emphasis has been placed on the measurement of the diffusion of drugs, alone or in combination with carrier molecules for enhanced solubility and facilitated transport. These studies have provided detailed comprehensive information—both kinetic and thermodynamic—for the design and operation of systems for the controlled release and delivery of drugs. Cyclodextrins are among the most important carriers used in these systems. The basis for their popularity is the ability of these materials to solubilize poorly soluble drugs, generally resulting in striking increases in their water solubilities. The techniques used in these investigations include pulse voltammetry, nuclear magnetic resonance (NMR) and Raman spectroscopy, ultrasonic relaxation, and dissolution kinetics. Transport in these systems is a mutual diffusion process involving coupled fluxes of drugs and carrier molecules driven by concentration gradients. Owing to a strong association in these multicomponent systems, it is not uncommon for a diffusing solute to drive substantial coupled fluxes of other solutes, mixed electrolytes, or polymers. Thus, diffusion data, including cross-diffusion coefficients for coupled transport, are essential in order to understand the rates of many processes involving mass transport driven by chemical concentration gradients, as crystal growth and dissolution, solubilization, membrane transport, and diffusion-limited chemical reactions are all relevant to the design of controlled-release systems. While numerous studies have been carried out on these systems, few have considered the transport behavior for controlled-release systems. To remedy this situation, we decided to measure mutual diffusion coefficients for coupled diffusion in a variety of drug–carrier solutions. In summary, the main objective of the present work was to understand the physical chemistry of carrier-mediated transport phenomena in systems of controlled drug release.

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pH-responsive magnetic micelles gelatin-g-poly(NIPAAm-co-DMAAm-co-UA)-g-dextran/Fe3O4 as a hydrophilic drug carrier

RSC Advances ◽

10.1039/c7ra01633f ◽

2017 ◽

Vol 7 (45) ◽

pp. 28207-28212 ◽

Cited By ~ 4

Author(s):

Chao-Ming Su ◽

Chen-Yu Huang ◽

Yao-Li Chen ◽

Tzong-Rong Ger

Keyword(s):

Controlled Release ◽

Drug Carrier ◽

Magnetic Targeting ◽

Ph Responsive ◽

Hydrophilic Drug

In the study, pH-selective magnetic targeting micelle, Gelatin-g-poly(NIPAAm-co-DMAAm-co-UA)-g-dextran/Fe3O4 (GPDF), has been synthesized for controlled release of a hydrophilic insulin-promoting factor, nicotinamide.

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The Current Research Status of PLGA as Drug and Gene Carrier

Journal of Nano Research ◽

10.4028/www.scientific.net/jnanor.42.80 ◽

2016 ◽

Vol 42 ◽

pp. 80-91 ◽

Cited By ~ 1

Author(s):

Ji Wei Wu ◽

Guo Hua Li ◽

Shu Qin Cui ◽

Jing He Wang ◽

Xiang Ling Gu ◽

...

Keyword(s):

Immune Response ◽

Surface Modification ◽

Controlled Release ◽

Glycolic Acid ◽

Drug Carrier ◽

Synthetic Methods ◽

Carrier System ◽

Carrier Materials ◽

Controlled Release System ◽

Drug Carrier System

PLGA, poly (lactic-co-glycolic-acid), is a kind of biodegradable functional macromolecular organic compounds. PLGA, certified by the Food and Drug Administration (FDA), possesses desirable features of biocompatibility, nontoxicity and no immune response, and is being widely applied to human clinical medical research. Because of its biodegradability, simple synthetic methods, controllability of degrading rate and desirable plasticity, PLGA was applied in large quantity into the carrier materials which is to control the release in recent years, gradually propelling PLGA microsphere controlled release system to be the most ideal drug-carrier system at present. As the carrier of drug and genes, PLGA is mainly researched on its features as the carrier, synthetic methods, different surface modification methods, and the applications on different drugs, genetic treatments and genetic vaccines.

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