Improvement of survival in C6 rat glioma model by a sustained drug release from localized PLGA microspheres in a thermoreversible hydrogel

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.

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Formulation and Evaluation of Chitosan-Polyaniline Nanocomposites for Controlled Release of Anticancer Drug Doxorubicin

International Journal of Drug Delivery Technology ◽

10.25258/ijddt.v8i2.13874 ◽

2018 ◽

Vol 8 (2) ◽

Author(s):

Dillip Kumar Behera ◽

Kampal Mishra ◽

Padmolochan Nayak

Keyword(s):

Tensile Strength ◽

Drug Release ◽

Nanocomposite Films ◽

Casting Method ◽

Sustained Drug Release ◽

In Vitro Drug Release ◽

Clay Particles ◽

Solution Casting Method ◽

Nanoclay Content

In this present work, chitosan (CS) crosslink with polyaniline (PANI) with montmorilonite (MMT) called as (CSPANI/MMT) and CS crosslink with PANI without MMT called as (CS-PANI) were prepared by employing the solution casting method. Further the formation of nanocomposites CS-PANI/MMT and CS-PANI were investigated using XRD, FTIR, SEM and tensile strength. Water uptake and swelling ratio of the CS-PANI and CS-PANI/MMT were found to decrease with increase in concentration of clay. Mechanical properties of the CS-PANI and CS-PANI/MMT were assessed in terms of tensile strength and extensibility using texture analyzer. Increase in tensile strength and reduction in extensibility was reported with increase in the nanoclay content. In vitro drug release study on CS-PANI and CS-PANI/MMT indicated pronounced sustained release of doxorubicin by the incorporation of clay particles in the CS polymer matrix. Overall CSPANI/MMT nanocomposite films exhibited improved mechanical and sustained drug release properties than CS-PANI.

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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.

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Design and Evaluation of Long Acting Biodegradable PLGA Microspheres for Ocular Drug Delivery

Nanoscience &Nanotechnology-Asia ◽

10.2174/2210681210666191223144755 ◽

2019 ◽

Vol 10 ◽

Author(s):

Anjali Pandya ◽

Rajani Athawale ◽

Durga Puro ◽

Geeta Bhagwat

Keyword(s):

Particle Size ◽

Drug Release ◽

Degradation Products ◽

Ex Vivo ◽

Research Work ◽

Entrapment Efficiency ◽

Rational Approach ◽

Plga Microspheres ◽

Long Acting

Background: The research work involves development of PLGA biodegradable microspheres loaded with dexamethasome for intraocular delivery. Objective: To design and evaluate long acting PLGA microspheres for ocular delivery of dexamethasone. Method: Present formulation involves the development of long acting dexamethasone loaded microspheres composed of a biodegradable controlled release polymer, Poly(D, L- lactide-co-glycolide) (PLGA), for the treatment of posterior segment eye disorders intravitreally. PLGA with monomer ratio of 50:50 of lactic acid to glycolic acid was used to achieve a drug release up to 45 days. Quality by Design approach was utilized for designing the experiments. Single emulsion solvent evaporation technique along with high pressure homogenization was used to facilitate formation of microspheres. Results: Particle size evaluation, drug content and drug entrapment efficiency were determined for the microspheres. Particle size and morphology was observed using Field Emission Gun-Scanning Electron Microscopy (FEG-SEM) and microspheres were in the size range of 1-5 μm. Assessment of drug release was done using in vitro studies and transretinal permeation was observed by ex vivo studies using goat retinal tissues. Conclusion: Considering the dire need for prolonged therapeutic effect in diseases of the posterior eye, an intravitreal long acting formulation was designed. Use of biodegradable polymer with biocompatible degradation products was a rational approach to achieve this aim. Outcome from present research shows that developed microspheres would provide a long acting drug profile and reduce the frequency of administration thereby improving patient compliance.

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Computational studies on self-assembled paclitaxel structures: Templates for hierarchical block copolymer assemblies and sustained drug release

Biomaterials ◽

10.1016/j.biomaterials.2009.08.022 ◽

2009 ◽

Vol 30 (33) ◽

pp. 6556-6563 ◽

Cited By ~ 69

Author(s):

Xin D. Guo ◽

Jeremy P.K. Tan ◽

Sung H. Kim ◽

Li J. Zhang ◽

Ying Zhang ◽

...

Keyword(s):

Block Copolymer ◽

Drug Release ◽

Computational Studies ◽

Sustained Drug Release ◽

Self Assembled

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Adhesive Hemostatic Conducting Injectable Composite Hydrogels with Sustained Drug Release and Photothermal Antibacterial Activity to Promote Full‐Thickness Skin Regeneration During Wound Healing

Small ◽

10.1002/smll.201900046 ◽

2019 ◽

Vol 15 (12) ◽

pp. 1900046 ◽

Cited By ~ 198

Author(s):

Yongping Liang ◽

Xin Zhao ◽

Tianli Hu ◽

Baojun Chen ◽

Zhanhai Yin ◽

...

Keyword(s):

Wound Healing ◽

Antibacterial Activity ◽

Drug Release ◽

Skin Regeneration ◽

Full Thickness ◽

Sustained Drug Release ◽

Composite Hydrogels ◽

Full Thickness Skin ◽

Thickness Skin

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The Impact of Gelatin on the Pharmaceutical Characteristics of Fucoidan Microspheres with Posaconazole

Materials ◽

10.3390/ma14154087 ◽

2021 ◽

Vol 14 (15) ◽

pp. 4087

Author(s):

Marta Szekalska ◽

Aleksandra Citkowska ◽

Magdalena Wróblewska ◽

Katarzyna Winnicka

Keyword(s):

Antifungal Activity ◽

Drug Release ◽

Spray Drying ◽

Fungal Infections ◽

Drug Loading ◽

High Surface ◽

Vaginal Fluid ◽

Sustained Drug Release ◽

Candida Spp ◽

The Impact

Fungal infections and invasive mycoses, despite the continuous medicine progress, are an important globally therapeutic problem. Multicompartment dosage formulations (e.g., microparticles) ensure a short drug diffusion way and high surface area of drug release, which as a consequence can provide improvement of therapeutic efficiency compared to the traditional drug dosage forms. As fucoidan is promising component with wide biological activity per se, the aim of this study was to prepare fucospheres (fucoidan microparticles) and fucoidan/gelatin microparticles with posaconazole using the one-step spray-drying technique. Pharmaceutical properties of designed fucospheres and the impact of the gelatin addition on their characteristics were evaluated. An important stage of this research was in vitro evaluation of antifungal activity of developed microparticles using different Candida species. It was observed that gelatin presence in microparticles significantly improved swelling capacity and mucoadhesiveness, and provided a sustained POS release. Furthermore, it was shown that gelatin addition enhanced antifungal activity of microparticles against tested Candida spp. strains. Microparticles formulation GF6, prepared by the spray drying of 20% fucoidan, 5% gelatin and 10% Posaconazole, were characterized by optimal mucoadhesive properties, high drug loading and the most sustained drug release (after 8 h 65.34 ± 4.10% and 33.81 ± 5.58% of posaconazole was dissolved in simulated vaginal fluid pH 4.2 or 0.1 M HCl pH 1.2, respectively).

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