scholarly journals A Long-Acting Curcumin Nanoparticle/In Situ Hydrogel Composite for the Treatment of Uveal Melanoma

Pharmaceutics ◽  
2021 ◽  
Vol 13 (9) ◽  
pp. 1335
Author(s):  
Lingxiao Xie ◽  
Weizhou Yue ◽  
Khaled Ibrahim ◽  
Jie Shen
Keyword(s):  
Uveal Melanoma ◽  
Cancer Progression ◽  
Hydrogel Composite ◽  
Medical Need ◽  
Sustain Release ◽  
Effective Inhibition ◽  
In Situ Hydrogel ◽  
Long Acting ◽  
In Situ Gelling

Uveal melanoma (UM) is the most common primary intraocular tumor in adults with high mortality. In order to improve prognosis and survival of UM patients, it is critical to inhibit tumor progression and metastasis as early as possible after the initial presentation/diagnosis of the disease. Sustained local delivery of antitumor therapeutics in the posterior region can potentially achieve long-term UM inhibition, improve target therapeutic delivery to the posterior segments, as well as reduce injection frequency and hence improved patient compliance. To address the highly unmet medical need in UM therapy, a bioinspired in situ gelling hydrogel system composed of naturally occurring biopolymers collagen and hyaluronic acid was developed in the present research. Curcumin with anti-cancer progression, anti-metastasis effects, and good ocular safety was chosen as the model therapeutic. The developed in situ gelling delivery system gelled at 37 °C within two minutes and demonstrated excellent biocompatibility and slow degradation. The curcumin-loaded nanoparticle/hydrogel composite was able to sustain release payload for up to four weeks. The optimized nanoparticle/hydrogel composite showed effective inhibition of human UM cell proliferation. This novel nanoparticle/in situ hydrogel composite demonstrated a great potential for the treatment of the rare and devastating intraocular cancer.

scholarly journals Bimatoprost loaded nanovesicular long-acting sub-conjunctival in-situ gelling implant: In vitro and in vivo evaluation

2019 ◽  
Vol 103 ◽  
pp. 109730 ◽  
Author(s):  
Monika Yadav ◽  
Ana Guzman-Aranguez ◽  
Maria J. Perez de Lara ◽  
Mandeep Singh ◽  
Joga Singh ◽  
...  
Keyword(s):  
In Vivo Evaluation ◽  
Long Acting ◽  
In Situ Gelling

Preliminary Characterization of Hydrogel Composite Alginate/PVA/r-GO as an Injectable Materials for Medical Applications

2019 ◽  
Vol 964 ◽  
pp. 161-167
Author(s):  
Amaliya Rasyida ◽  
Yohannes Marudut Tua Silaen ◽  
Sigit Tri Wicaksono ◽  
Hosta Ardyananta ◽  
Haniffudin Nurdiansah ◽  
...  
Keyword(s):  
Poly Vinyl Alcohol ◽  
Curing Time ◽  
Medical Purpose ◽  
Alginate Hydrogel ◽  
Hydrogel Composite ◽  
Injection Process ◽  
Reduced Graphene ◽  
In Situ Gelling

The study aimed to synthesize alginate hydrogel-based composites which could be injected for medical purpose and can be cured in situ gelling after the injection process. The effect of reduced graphene oxide (r-GO) addition on Alginate /poly (vinyl alcohol) (PVA) hydrogel to physical properties were evaluated. Synthesis of hydrogel Alginate/PVA/r-GO composite was previously performed by production of r-GO using Hummer method. The composition of r-GO used in composite hydrogel was 0.4, 0.8, 1.2 and 1.6% wt. The sample was then characterized using XRD, FTIR, and analyzed perform with its curing time, injectable performance, swelling ratio, and water content.

scholarly journals Development, Optimization, and In Vitro Evaluation of Novel Oral Long-Acting Resveratrol Nanocomposite In-Situ Gelling Film in the Treatment of Colorectal Cancer

Gels ◽  
2021 ◽  
Vol 7 (4) ◽  
pp. 276
Author(s):  
Shadab Md ◽  
Samaa Abdullah ◽  
Nabil A. Alhakamy ◽  
Waleed S. Alharbi ◽  
Javed Ahmad ◽  
...  
Keyword(s):  
Colorectal Cancer ◽  
Drug Release ◽  
Encapsulation Efficiency ◽  
Interleukin 1 ◽  
B Cell Lymphoma ◽  
Enzyme Linked Immunosorbent Assay ◽  
Drug Release Profile ◽  
Long Acting ◽  
In Situ Gelling

this study aimed to develop and evaluate sustained-release (SR) long-acting oral nanocomposites in-situ gelling films of resveratrol (Rv) to treat colorectal cancer. In these formulations, Rv-Soy protein (Rv-Sp) wet granules were prepared by the kneading method and then encapsulated in the sodium alginate (NA) dry films. The prepared nanocomposite in-situ gels films were characterized using dynamic light scattering, Fourier-transform infrared spectroscopy, X-ray diffraction, and scanning electron microscopy. The optimized formulations were further evaluated based on drug encapsulation efficiency, pH-drug release profile, swelling study, and storage time effects. The optimized formulation was tested for its anticancer activity against colorectal cancer cells using the cytotoxicity assessment, apoptosis testing, cell cycle analysis, gene expression analysis, and protein estimation by the reverse-transcriptase polymerase chain reaction and enzyme-linked immunosorbent assay methods, respectively. The optimum film showed encapsulation efficiency of 97.87% ± 0.51 and drug release of 14.45% ± 0.043 after 8 h. All physiochemical characterizations confirmed, reasoned, and supported the drug release experiment’s findings and the encapsulation assay. The Rv nanocomposite formulation showed concentration-dependent cytotoxicity enhanced apoptotic activity as compared to free Rv (p < 0.05). In addition, Rv nanocomposite formulation caused a significant increase in Bcl-2-associated protein X (Bax) and a decrease in expression of B-cell lymphoma 2, interleukin 1 beta, IL-6, and tumor necrosis factor-alpha (Bcl2, IL-1β, IL-6, and TNF-α respectively) compared to that of free Rv in HCT-116 cells. These results suggest that long-acting Rv nanocomposite gels could be a promising agent for colorectal cancer treatment.

scholarly journals Formulation, Ex-Vivo and Preclinical In-Vivo Studies of Combined pH and Ion-Sensitive Ocular Sustained In Situ Hydrogel of Timolol Maleate for the Treatment of Glaucoma

2020 ◽  
Vol 11 (1) ◽  
pp. 8242-8265
Keyword(s):  
Drug Release ◽  
Physiological Condition ◽  
Controlled Drug Release ◽  
Gellan Gum ◽  
Class I ◽  
Timolol Maleate ◽  
In Situ Hydrogel ◽  
In Situ Gelling ◽  
Carbopol 934P

The aim of the present research work was to develop safe, effective, and stable in situ hydrogel for the ophthalmic drug delivery using the combination of ion-responsive polymer gellan gum and pH-sensitive polymer carbopol 934P to treat glaucoma. Background: Timolol maleate is a BCS class I drug used as the first line of treatment in open-angle glaucoma. The rapid precorneal elimination of conventional formulation containing class I drugs exhibits poor therapeutic effect and bioavailability. So, in situ gelling system was formulated and characterized. Methods: Box-Behnken design was used to statistically optimize the formulation parameters and evaluate the effects of formulation attributes, namely concentration of gellan gum (X1), the concentration of carbopol 934P (X2) and concentration of benzododecenium bromide (X3) on selected critical quality attributes (Y1-Y7). Trial run data were statistically analyzed using the polynomial equation and response surface plots. Optimized formulation was selected based on desirability function, design space, and was further characterized and compared with the marketed formulation. Results: The concentration of both polymers showed a synergistic positive impact on viscosity at the non-physiological and physiological conditions. Trial runs showed controlled drug release with diffusion-controlled mechanism and good mucoadhesive strength due to the presence of Carbopol 934P. The preservative benzododecenium bromide showed the ability to enhance trans-corneal permeation. The optimized formulation has appeared as a clear solution at the non-physiological condition and clear gel at the physiological condition with an acceptable pH range of 5-6. Other quality attributes like rheological properties, gelling capacity, texture analysis, Isotonicity, contact angle, sterility, antimicrobial efficacy, and stability were found in desires values for the ocular application. The safety of in situ gel for human use was confirmed by ocular irritation and histopathology studies in the rabbit eyes. The intraocular pressure (IOP) reduction with optimized formulation was found comparable and less fluctuating compared to ophthalmic gel-forming marketed solution of timolol maleate (TIMOPTIC-XE®). Conclusion: The cross-linking between Carbopol 934P with Gellan gum in the formation showed more viscous gelling at the physiological condition to provide long pre-corneal residence time. The optimized formulation exhibited all the desirable attributes of an ideal ophthalmic in situ gelling formulation, exhibited in-vitro controlled drug release, good gelling capacity, and was found to be stable and non-irritant to the eye.

Novel Formulation Development and Evaluation of Nanoparticles Based in Situ Gelling System for The Ophthalmic Delivery of Ciprofloxacin Hydrochloride

2015 ◽  
Vol 5 (4) ◽  
Author(s):  
Kranti Singh ◽  
Surajpal Verma ◽  
Shyam Prasad ◽  
Indu Bala
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Drug Loading ◽  
In Vitro Release ◽  
Formulation Development ◽  
Ciprofloxacin Hydrochloride ◽  
Potential Value ◽  
The Mean ◽  
In Situ Gelling

Ciprofloxacin hydrochloride loaded Eudragit RS100 nanoparticles were prepared by using w/o/w emulsification (multiple emulsification) solvent evaporation followed by drying of nanoparticles at 50°C. The nanoparticles were further incorporated into the pH-triggered in situ gel forming system which was prepared using Carbopol 940 in combination with HPMC as viscosifying agent. The developed nanoparticles was evaluated for particle size, zeta potential value and loading efficiency; nanoparticle incorporated in situ gelling system was evaluated for pH, clarity, gelling strength, rheological studies, in-vitro release studies and ex-vivo precorneal permeation studies. The nanopaticle showed the mean particle size varying between 263.5nm - 325.9 nm with the mean zeta potential value of -5.91 mV to -8.13 mV and drug loading capacity varied individually between 72.50% to 98.70% w/w. The formulation was clear with no suspended particles, showed good gelling properties. The gelling was quick and remained for longer time period. The developed formulation was therapeutically efficacious, stable and non-irritant. It provided the sustained release of drug over a period of 8-10 hours.

scholarly journals Development of In Situ Self-Assembly Nanoparticles to Encapsulate Lopinavir and Ritonavir for Long-Acting Subcutaneous Injection

Pharmaceutics ◽  
2021 ◽  
Vol 13 (6) ◽  
pp. 904
Author(s):  
Irin Tanaudommongkon ◽  
Asama Tanaudommongkon ◽  
Xiaowei Dong
Keyword(s):  
Sustained Release ◽  
Trough Concentration ◽  
Self Assembly ◽  
Subcutaneous Injection ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Long Acting

Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.

scholarly journals Poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) Copolymers for the Formulation of In Situ Forming Depot Long-Acting Injectables

Pharmaceutics ◽  
2021 ◽  
Vol 13 (5) ◽  
pp. 605
Author(s):  
Marie-Emérentienne Cagnon ◽  
Silvio Curia ◽  
Juliette Serindoux ◽  
Jean-Manuel Cros ◽  
Feifei Ng ◽  
...  
Keyword(s):  
Ethylene Glycol ◽  
Surface Erosion ◽  
Sustained Delivery ◽  
Trimethylene Carbonate ◽  
Poly Ethylene Glycol ◽  
In Situ Forming ◽  
Poly Ethylene ◽  
Long Acting

This article describes the utilization of (methoxy)poly(ethylene glycol)-b-poly(1,3-trimethylene carbonate) ((m)PEG–PTMC) diblock and triblock copolymers for the formulation of in situ forming depot long-acting injectables by solvent exchange. The results shown in this manuscript demonstrate that it is possible to achieve long-term drug deliveries from suspension formulations prepared with these copolymers, with release durations up to several months in vitro. The utilization of copolymers with different PEG and PTMC molecular weights affords to modulate the release profile and duration. A pharmacokinetic study in rats with meloxicam confirmed the feasibility of achieving at least 28 days of sustained delivery by using this technology while showing good local tolerability in the subcutaneous environment. The characterization of the depots at the end of the in vivo study suggests that the rapid phase exchange upon administration and the surface erosion of the resulting depots are driving the delivery kinetics from suspension formulations. Due to the widely accepted utilization of meloxicam as an analgesic drug for animal care, the results shown in this article are of special interest for the development of veterinary products aiming at a very long-term sustained delivery of this therapeutic molecule.

scholarly journals Efficacy and Safety of Azelaic Acid Nanocrystal-Loaded In Situ Hydrogel in the Treatment of Acne Vulgaris

Pharmaceutics ◽  
2021 ◽  
Vol 13 (4) ◽  
pp. 567
Author(s):  
Ivona Tomić ◽  
Sandra Miočić ◽  
Ivan Pepić ◽  
Dubravka Šimić ◽  
Jelena Filipović-Grčić
Keyword(s):  
Azelaic Acid ◽  
Controlled Trial ◽  
Acne Vulgaris ◽  
Topical Therapy ◽  
Adverse Event Rate ◽  
Double Blind ◽  
Inflammatory Lesions ◽  
First Choice ◽  
In Situ Hydrogel

Acne vulgaris is a common, multifactorial, inflammatory skin disease affecting the pilosebaceous unit. Topical therapy is the first choice in the treatment of mild to moderate acne, and azelaic acid (AZA) is one of the most commonly used drugs. The aim of this study was to evaluate the safety and efficacy of a low-dose azelaic acid nanocrystal (AZA-NC) hydrogel in the treatment of mild to moderate facial acne. The study was designed as a double-blind, randomized controlled trial. Patients were randomized to treatment with AZA-NC hydrogel, 10%, or AZA cream, 20%, administered in quantities of approximately 1 g twice daily for 8 weeks. Efficacy of therapy was measured by the number of lesions and safety by the frequency and severity of adverse events. At week 8, the success rate of treatment with AZA-NC hydrogel, 10%, was 36.51% (p < 0.001) versus 30.37% (p < 0.001) with AZA cream. At week 8, treatment with AZA-NC hydrogel, 10%, resulted in a significant reduction in total inflammatory lesions from baseline of 39.15% (p < 0.001) versus 33.76% (p < 0.001) with AZA cream, and a reduction in non-inflammatory lesions from baseline of 34.58% (p < 0.001) versus 27.96% (p < 0.001) with AZA cream, respectively. The adverse event rate was low and mostly mild.

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