scholarly journals Acid-Treated Water-Soluble Chitosan Suitable for Microneedle-Assisted Intracutaneous Drug Delivery

Pharmaceutics ◽  
2019 ◽  
Vol 11 (5) ◽  
pp. 209 ◽  
Author(s):  
Ajeesh Chandrasekharan ◽  
Young Jun Hwang ◽  
Keum-Yong Seong ◽  
Samdae Park ◽  
Sodam Kim ◽  
...  

Chitosan has been widely used as a nature-derived polymeric biomaterial due to its high biocompatibility and abundance. However, poor solubility in aqueous solutions of neutral pH and multiple fabrication steps for the molding process limit its application to microneedle technology as a drug delivery carrier. Here, we present a facile method to prepare water-soluble chitosan and its application for sustained transdermal drug delivery. The water-soluble chitosan was prepared by acid hydrolysis using trifluoroacetic acid followed by dialysis in 0.1 M NaCl solutions. We successfully fabricated bullet-shaped microneedle (MN) arrays by the single molding process with neutral aqueous chitosan solutions (pH 6.0). The chitosan MN showed sufficient mechanical properties for skin insertion and, interestingly, exhibited slow dissolving behavior in wet conditions, possibly resulting from a physical crosslinking of chitosan chains. Chitosan MN patches loading rhodamine B, a model hydrophilic drug, showed prolonged release kinetics in the course of the dissolving process for more than 72 h and they were found to be biocompatible to use. Since the water-soluble chitosan can be used for MN fabrication in the mild conditions (neutral pH and 25 °C) required for the loading of bioactive agents such as proteins and achieve a prolonged release, this biocompatible chitosan MN would be suitable for sustained transdermal drug delivery of a diverse range of drugs.

2018 ◽  
Vol 10 (1) ◽  
pp. 67
Author(s):  
Bhawana Sethi ◽  
Rupa Mazumder

Objective: The present work was aimed at preparation of transdermal patches by a solvent casting method using a varying concentration of polymers i.e. methocel (K15 and K100), ethocel (4 and 10), gelatin, chitosan, eudragit (RL and RS) grade using plasticizer (glycerin and propylene glycol).Methods: The ratio of drug to polymers and plasticizer was varied and the effect of formulation variables was studied. Prepared transdermal patches were evaluated for physicochemical properties, in-vitro permeation studies, content uniformity, primary skin irritation studies and FT-IR studies.Results: The formulated transdermal patch by using Methocel K 100 M showed good physical properties. The average weight of patches prepared using glycerin as a plasticizer were ranged from 42.33-67.00 mg and propylene glycol as a plasticizer were ranged from 40.67-67.67 mg. The percentage moisture absorption varies from 1.76 to 10.73 for patches formulated using glycerin and 2.28 to 7.97 for propylene glycol patches. The percentage moisture loss from patches prepared using glycerin was ranged from 2.75 to 11.54 and 2.87 to 12.02 from propylene glycol. The water vapour transmission rate from patches prepared using glycerin was ranged from 0.25 to 0.92 and 0.41 to 1.76. The formulated patch showed the acceptable quantity of medicament ranged from (100.20-101.05%). This result met the test content uniformity as per BP (85% to 115%). According to that, the drug was consistent throughout the patches. The formulation PGD is considered as the best formulation, since it shows a maximum in vitro drug release as 43.75 % at 24 h. The drug release kinetics studied showed that the majority of formulations was following zero order.Conclusion: In conclusion, controlled release transdermal drug delivery system patches of aliskiren can be prepared using polymer combinations, with a different plasticizer. The release rate of drug depends upon the polymer. However, release kinetics followed zero order.


Author(s):  
Sanjoy Das ◽  
Malay K. Das

Objective: Site-specific drug delivery into the colonic region is extremely fascinating for local treatment of various colonic diseases like ulcerative colitis, colon cancer but it should be capable of saving the drug from hydrolysis and degradation. The present study reports the application of jackfruit seed starch and its thiol derivative as a drug delivery carrier for the colon. Methods: The starch was extracted from the jackfruit seeds by water extraction method and modified by the esterification reaction with thioglycolic acid. The thiolated starch was characterized for morphology, functional and flow properties. The safety profile of the thiolated starch was confirmed by acute toxicity study in a mice model as per OECD guidelines 423. The microspheres based on thiolated starch were prepared by ionic gelation method incorporating Ibuprofen as a model drug. The prepared microspheres were characterized for particle size, drug entrapment efficiency, drug loading, compatibility study, surface morphology, in vitro drug release and release kinetics. Results: The result attributed that starch was successfully modified by the thiolation with a degree of substitution of 3.30. The size of prepared microspheres ranges from 825.5±4.58 to 857±6.24 µm, the entrapment efficiencies ranges from 69.23±1.19 to 76.15±0.83 % and the drug loading capacity ranges from 17.75±0.30 to 46.05±0.49 %. The FT-IR, DSC and XRD studies confirmed that there is no interaction within drug and excipients. The thiolated starch microspheres show the maximum release of drug at pH 7.4 in the presence of rat caecal content as compared to pH 1.2 and pH 6.8 for up to 24 h and are following first order release kinetics. Conclusion: These results suggest the application of thiolated jackfruit seed starch could be promising as a long-term drug delivery carrier for the colon.


2021 ◽  
Author(s):  
Hirotada Hirama ◽  
Yuya Ishikura ◽  
Shinya Kano ◽  
Masanori Hayase ◽  
Harutaka Mekaru

This study presents an alternative to cross-linking for the preparation of monodispersed polymer microcapsules made from water-soluble and biocompatible sodium hyaluronate (SH). Water was removed from monodispersed drug-containing SH droplets...


2021 ◽  
Vol 17 ◽  
Author(s):  
Surya Goel ◽  
Vijay Agarwal ◽  
Monika Sachdeva

Background: Nanocrystals have been found as potent, beneficial and advantageous nanocarrier systems for ameliorating the solubility, bioavailability and permeability of those drug candidates that are less water-soluble and permeable. Such an approach possesses many complications that require more research work. Objective: The main objective of the manuscript is to prepare a review on all the aspects of nanocrystals, including their advantages, recent advancements, preparation methods, recent patents, marketed products and some patents related to their characterization techniques. Methods: This manuscript has been accrued through the help of online and offline journals, books, and from some other accessible sources. This field involves new developments or inventions in the novel nanocarrier system. Results: Nanocrystals have been found to exhibit better potentiality sorting out different problems like poor drug absorption, drug-associated side effects, and targeted drug delivery. In the last decade, these nanocarriers have been opted for resolving the problem of production due to less soluble drugs. By conducting more researches, this field can be more beneficial to the health sector. Conclusion: Nanocrystals significantly to deliver several drugs via different routes like topical, oral ophthalmic, pulmonary and parenteral. This manuscript substantially shows the applicability and importance of nanocrystals as a drug delivery carrier to treat various health issues.


2011 ◽  
Vol 18 (4) ◽  
pp. 798-803 ◽  
Author(s):  
Tanasait Ngawhirunpat ◽  
Narumon Worachun ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Suwannee Panomsuk

2013 ◽  
Vol 19 (2) ◽  
pp. 164-172 ◽  
Author(s):  
Ponwanit Charoenputtakhun ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat

2012 ◽  
Vol 8 ◽  
pp. 2091-2099 ◽  
Author(s):  
Francesco Trotta ◽  
Marco Zanetti ◽  
Roberta Cavalli

Cyclodextrin-based nanosponges, which are proposed as a new nanosized delivery system, are innovative cross-linked cyclodextrin polymers nanostructured within a three-dimensional network. This type of cyclodextrin polymer can form porous insoluble nanoparticles with a crystalline or amorphous structure and spherical shape or swelling properties. The polarity and dimension of the polymer mesh can be easily tuned by varying the type of cross-linker and degree of cross-linking. Nanosponge functionalisation for site-specific targeting can be achieved by conjugating various ligands on their surface. They are a safe and biodegradable material with negligible toxicity on cell cultures and are well-tolerated after injection in mice. Cyclodextrin-based nanosponges can form complexes with different types of lipophilic or hydrophilic molecules. The release of the entrapped molecules can be varied by modifying the structure to achieve prolonged release kinetics or a faster release. The nanosponges could be used to improve the aqueous solubility of poorly water-soluble molecules, protect degradable substances, obtain sustained delivery systems or design innovative drug carriers for nanomedicine.


2013 ◽  
Vol 2013 ◽  
pp. 1-6 ◽  
Author(s):  
Basem A. Moosa ◽  
Afnan Mashat ◽  
Wengang Li ◽  
Karim Fhayli ◽  
Niveen M. Khashab

Polystyrene-block-polyvinylpyridine (PS-b-P4VP) polypseudorotaxanes with cucurbit[7]urils (CB[7]) were prepared from water soluble PS-b-P4VPH+polymer and CB[7] in aqueous solution at room temperature. At acidic and neutral pH, the pyridinium block of PS-b-P4VP is protonated (PS-b-P4VPH+) pushing CB[7] to preferably host the P4VP block. At basic pH (pH 8), P4VP is not charged and thus is not able to strongly complex CB[7]. This phenomenon was verified further by monitoring the release of pyrene, a hydrophobic cargo model, from a PS-b-P4VPH+/CB[7] micellar membrane. Release study of UV active pyrene from the membrane at different pH values revealed that the system is only operational under basic conditions and that the host-guest interaction of CB[7] with P4VPH+significantly slows down cargo release.


2012 ◽  
Vol 506 ◽  
pp. 441-444 ◽  
Author(s):  
Narumon Worachun ◽  
Praneet Opanasopit ◽  
Theerasak Rojanarata ◽  
Tanasait Ngawhirunpat

The aim of this study was to prepare microemulsion for transdermal drug delivery of ketoprofen (KP). The physicochemical and chemical properties of microemulsion were evaluated. The microemulsion were composed of isopropyl myristate (IPM) as oil phase, water, PEG40-hydrogenated castor oil (Cremophor® RH40) as surfactant and PEG400 as co-surfactant, and the surfactant: co-surfactant ratio used was 1:1. The viscosity, droplet size, pH, conductivity of microemulsion and skin permeation of KP through shed snake skin were evaluated. The particle size, viscosity and conductivity of microemulsions were in the range of 172-468 nm, 234.82-1067.35 cP and 6.80-20.87µS/cm, respectively. The ratio of IPM and surfactant mixture played an important role on KP loading capacity of microemulsions formulation and skin permeation of KP. While amount of surfactant increased, the loading capacity of KP increased, but the skin permeation of KP decreased. The results suggested that the novel microemulsion system composed of IPM, water, Cremophor® RH40:PEG400 (ratio 1:1) can be applied for using as a transdermal drug delivery carrier.


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