Synthesis of biogenic gold nano conjugate for increased efficacy and sustained drug release profile of saquinavir

Abstract Microneedles (MNs) provide a minimally invasive alternative to intravitreal injections and a promising means to sustainable ocular drug delivery. To optimize the sustained drug release profile and to ease the administration of the MN array to the eye, the number of MNs in an MN array and their layout need to be carefully selected. In this study, the drug release kinetics of MN arrays with varying numbers of MNs (8, 12, and 16) is studied over a four-week period. The MN arrays show a much more uniform drug release profile than the single injections. Only the 16-needle MN array fully released all the amount of loaded drug at the end of the 4-week period. Both 8- and 12-needle arrays showed a steady release rate over the 4-week period, which is the longest sustained release duration that has been reported. Zero-order models are created to predict drug release profiles for the three MN arrays. It is estimated that the MN array with 8 needles can deliver the drug for up to 6 weeks. The models can be used to design MN arrays with a given targeted therapeutic index for sustained drug delivery.

Download Full-text

Poly(ε-caprolactone) nanocapsule carriers with sustained drug release: single dose for long-term glaucoma treatment

Nanoscale ◽

10.1039/c7nr03221h ◽

2017 ◽

Vol 9 (32) ◽

pp. 11754-11764 ◽

Cited By ~ 17

Author(s):

Chih-Hung Lee ◽

Yu-Jia Li ◽

Chih-Ching Huang ◽

Jui-Yang Lai

Keyword(s):

Single Dose ◽

Drug Release ◽

Release Profile ◽

Drug Release Profile ◽

Sustained Drug Release ◽

Glaucoma Treatment

The loading of pilocarpine in the poly(ε-caprolactone) nanocapsules exhibited a sustained drug release profile and effective pharmacological responses for glaucoma treatment.

Download Full-text

Studies on the Drug Loading and Release Profiles of Degradable Chitosan-Based Multilayer Films for Anticancer Treatment

Cancers ◽

10.3390/cancers12030593 ◽

2020 ◽

Vol 12 (3) ◽

pp. 593 ◽

Cited By ~ 6

Author(s):

Hyeongdeok Sun ◽

Daheui Choi ◽

Jiwoong Heo ◽

Se Yong Jung ◽

Jinkee Hong

Keyword(s):

Drug Release ◽

Multilayer Film ◽

Drug Loading ◽

Building Blocks ◽

Multilayer Films ◽

Release Profile ◽

Layer By Layer ◽

Drug Release Profile ◽

Sustained Drug Release ◽

Release Profiles

This study demonstrates the possibility of developing a rapidly degradable chitosan-based multilayer film for controlled drug release. The chitosan (CHI)-based multilayer nanofilms were prepared with three different types of anions, hyaluronic acid (HA), alginic acid (ALG) and tannic acid (TA). Taking advantage of the Layer-by-Layer (LBL) assembly, each multilayer film has different morphology, porosity and thickness depending on their ionic density, molecular structure and the polymer functionality of the building blocks. We loaded drug models such as doxorubicin hydrochloride (DOX), fluorescein isothiocyanate (FITC) and ovalbumin (Ova) into multilayer films and analyzed the drug loading and release profiles in phosphate-buffered saline (PBS) buffer with the same osmolarity and temperature as the human body. Despite the rapid degradation of the multilayer film in a high pH and salt solution, the drug release profile can be controlled by increasing the functional group density, which results in interaction with the drug. In particular, the abundant carboxylate groups in the CHI/HA film increased the loading amount of DOX and decreased rapid drug release. The TA interaction with DOX via electrostatic interaction, hydrogen bonding and hydrophobic interaction showed a sustained drug release profile. These results serve as principles for fabricating a tailored multilayer film for drug delivery application.

Download Full-text

Synthesis, Characterization and in-vitro drug release studies of a macromolecular prodrug of Didanosine.

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v2i2.8845 ◽

2010 ◽

Vol 2 (2) ◽

Author(s):

Neeraj Agrawal ◽

M.J. Chandrasekar ◽

U.V. Sara ◽

Rohini A.

Keyword(s):

Drug Release ◽

Drug Level ◽

Drug Release Profile ◽

Sustained Drug Release ◽

In Vitro Drug Release ◽

Alkaline Environment ◽

Stomach Acid ◽

Release Studies ◽

Macromolecular Prodrug

A macromolecular prodrug of didanosine (ddI) for oral administration was synthesized and evaluated for in-vitro drug release profile. Didanosine was first coupled to 2-hydroxy ethyl methacrylate (HEMA) through a succinic spacer to form HEMA-Suc-ddI monomeric conjugate which was subsequently polymerized to yield Poly(HEMA-Suc-ddI) conjugate. The structures of the synthesized compounds were characterized by FT-IR, Mass and 1H-NMR spectroscopy. The prodrug was subjected for in-vitro drug release studies in buffers of pH 1.2 and 7.4 mimicking the upper and lower GIT. The results showed that the drug release from the polymeric backbone takes place in a sustained manner over a period of 24 h and the amount of drug released was comparatively higher at pH 7.4 indicating that the drug release takes place predominantly at the alkaline environment of the lower GIT rather than at the acidic environment of the upper GIT. This pH dependent sustained drug release behavior of the prodrug may be capable of reducing the dose limiting toxicities by maintaining the plasma drug level within the therapeutic range and increasing t1/2 of ddI. Moreover, the bioavailability of the drug should be improved as the prodrug releases ddI predominantly in the alkaline environment which will reduce the degradation of ddI in the stomach acid.

Download Full-text

Anticancer Nano Formulation of Imatinib with Chitosan Polymer

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.9.1.10 ◽

2019 ◽

Vol 9 (01) ◽

pp. 58-64

Author(s):

Senthilnathan B ◽

Billy Graham R ◽

Chaarmila Sherin C ◽

Vivekanandan K ◽

Bhavya E

Keyword(s):

Drug Release ◽

Drug Targeting ◽

Bone Marrow Failure ◽

Lymphoblastic Leukemia ◽

Release Profile ◽

Nano Particles ◽

Drug Release Profile ◽

Study Results ◽

Mast Cell Disease ◽

Nano Formulation

Objective: Drug targeting is the capacity of the dosage form. In which the therapeutic agent acts specifically to desired site of action in the non-targeted tissue with the help of Nano particles is called as the drug targeting. IMATINIB is a used to treat cancer by chemo therapy. Cancers like chronic myeloid leukemia cancer (CML) and acute lymphoblastic leukemia cancer (ALL) and other specific types of gastrointestinal stromal cell tumor (GIST) systemic mast cell disease and Bone marrow failure disorder. It is administered by oral root. For ATP, Tyrosine kinase is act as a binding site. Methodology: The drug IMATINIB is loaded in the polymer chitosan, poly-(D) glucosamine is a bio compactible, bio degradable, nontoxic, antimicrobial and soluble in solvents. This preparation is done by emulsion-droplet coalescence method. Content of the Drug, Size of the particle and Zeta potential, Encapsulation efficiency and Drug release testing are described for this formulation in this study. Results: The Imatinib Nano particles were formulated and evaluated for its invitro drug release profile. Based on the invitro drug release profile of Imatinib nano particles formulation (INP1 – INP5) formulation INP3 was selected as the best formulation in which the particle size was 285.9nm. The invitro % drug release of INP3 formulation was 99.76 ± 0.82 and it was found to be the suitable formulation to manage the cancer. Conclusion: Hence it is concluded that the newly formulated controlled release nanoparticle drug delivery system of Imatinib may be idol and effective by allowing the drug to release continuously for 24 hrs.

Download Full-text

Development and Optimization of Sustained Release Moxifloxacin Hydrochloride Loaded Nanoemulsion for Ophthalmic Drug Delivery: A 32 Factorial Design Approach

Micro and Nanosystems ◽

10.2174/1876402912999200826111031 ◽

2020 ◽

Vol 12 ◽

Author(s):

Sagar R. Pardeshi ◽

Harshal A. Mistari ◽

Rakhi S. Jain ◽

Pankaj R. Pardeshi ◽

Rahul L. Rajput ◽

...

Keyword(s):

Drug Release ◽

Sustained Release ◽

Factorial Design ◽

Water Solubility ◽

Tween 80 ◽

Drug Release Profile ◽

Sustained Drug Release ◽

Bacterial Conjunctivitis ◽

Promising Alternative

Background: Moxifloxacin is a BCS class I drug used in the treatment of bacterial conjunctivitis and keratitis. Despite its high water solubility, it possesses limited bioavailability due to anatomical and physiological constraints associated with the eyes which required multiple administrations to achieve a therapeutic effect. Objective: In order to prolong drug release and to improve antibacterial efficacy for the treatment of bacterial keratitis and conjunctivitis, moxifloxacin loaded nanoemulsion was developed. Methods: The concentration of oil (oleic acid), surfactant (tween 80), and cosurfactant (propylene glycol) were optimized by employing a 3-level 2-factorial design of experiment for the development of nanoemulsion. The developed nanoemulsion was characterized by particle size distribution, viscosity, refractive index, pH, drug content and release, transmission electron microscopy (TEM), and antibacterial study. The compatibility of the drug with the excipients was accessed by Fourier transform infrared spectroscopy (FTIR). Result: The average globule size was found to be 198.20 nm. The TEM study reveals the globules were nearly spherical and are well distributed. In vitro drug release profile for nanoemulsion shown sustained drug release (60.12% at the end of 6 h) compared to drug solution, where complete drug released within 2 h. The antibacterial effectiveness of the drug-loaded nanoemulsion was improved against S. aureus compared with the marketed formulation. Conclusion: The formulated sustained release nanoemulsion could be a promising alternative to eye drop with improved patient compliance by minimizing dosing frequency with improved antibacterial activity.

Download Full-text

Swelling behaviour, rheological property and drug release profile of the anti-inflammatory drug metamizole sodium from xanthan gum–ZnO nanoparticles

Polymer Bulletin ◽

10.1007/s00289-020-03509-5 ◽

2021 ◽

Author(s):

Selcan Karakus ◽

Ezgi Tan ◽

Merve Ilgar ◽

Yeşim Müge Sahin ◽

Demet Sezgin Mansuroglu ◽

...

Keyword(s):

Drug Release ◽

Rheological Property ◽

Zno Nanoparticles ◽

Xanthan Gum ◽

Release Profile ◽

Drug Release Profile ◽

Swelling Behaviour ◽

Inflammatory Drug ◽

Anti Inflammatory ◽

Metamizole Sodium

Download Full-text

Effect of a co-processed excipient on the disintegration and drug release profile of ibuprofen tablets

Bio-Research ◽

10.4314/br.v18i1.7 ◽

2020 ◽

Vol 18 (1) ◽

Author(s):

BB Mohammed ◽

EJ John ◽

NK Ajuji

Keyword(s):

Drug Release ◽

Release Profile ◽

Angle Of Repose ◽

Oral Dosage ◽

Direct Compression ◽

Drug Release Profile ◽

Disintegration Time ◽

Crushing Strength ◽

Tablet Properties ◽

Spray Dried

Tablets at present, remain the most preferred oral dosage form because of many advantages they offer to formulators as well as physicians and patients. The objective of this work was to determine the effect of co-processing on the disintegration and drug-release profile of ibuprofen tablets prepared from a co-processed excipient. The co-processed excipient (CE) containing lactose, gelatin and mucin in the ratio 90:9:1 was prepared using co-fusion. The excipient was evaluated for its physicochemical properties and then used to formulate tablets with the addition of a disintegrant by direct compression. The tablets were evaluated for their tablet properties and compared with tablets prepared with cellactose- 80® (CEL) and spray dried lactose® (SDL) and a physical mix (PM) of the co-processed ingredient. Results from evaluation of CE showed that flow rate, angle of repose, Carr’s index and Hausner’s ratio were 5.28 g/sec, 20.30o, 23.75 % and 1.31, respectively. Tablets prepared with CE had friability (0%), crushing strength (5.25) KgF, disintegration time (3 mins) and T50% (2 mins). For CEL, friability (0.4 %), crushing strength (7.25) KgF, disintegration time (1 min) and T50% (2 mins); SDL, friability (1.57 %), crushing strength (7.50) KgF, disintegration time (4 mins) and T50% (2 mins) and PM, friability (2.38 %), crushing strength (5.00) KgF, disintegration time (1 min) and T50% (2 mins). In conclusion, the disintegration time and drug release profile for CE was not superior but compared favorably with CEL, SDL and PM.

Download Full-text