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 Development and Optimization of Chitosan-Hydroxypropyl Methylcellulose In Situ Gelling Systems for Ophthalmic Delivery of Bupivacaine Hydrochloride

Processes ◽  
2021 ◽  
Vol 9 (10) ◽  
pp. 1694
Author(s):  
Lăcrămioara Popa ◽  
Mihaela Violeta Ghica ◽  
Roxana Popescu ◽  
Teodora Irimia ◽  
Cristina-Elena Dinu-Pîrvu
Keyword(s):  
Drug Release ◽  
Hydroxypropyl Methylcellulose ◽  
Second Phase ◽  
Colloidal Systems ◽  
Drug Release Profile ◽  
Bupivacaine Hydrochloride ◽  
Ophthalmic Delivery ◽  
In Situ Gelling

The aim of this study was the development and optimization of chitosan and hydroxypropyl methylcellulose (HPMC) in situ gelling systems, loaded with bupivacaine hydrochloride for topical ocular administration. This study is based on the properties of two polymers: chitosan, which has mucoadhesive action and is a pH-sensitive polymer, but also the cellulose derivative hydroxypropyl methylcellulose, a thermosensitive polymer which has mucoadhesive properties and increases the viscosity of systems. The analysis and optimization of in situ gelling systems were performed based on an experimental design and response surface methodology. The following formulation parameters were considered: X1 = chitosan concentration (0.5%, 1%), X2 = HPMC E 5 LV concentration (2%, 5%) and X3 = Chitosan/HPMC E 5 LV ratio (1/1, 2/1). In addition, the parameters to be optimized were represented by the contact angle (CA (°)), viscosity and cumulative percentage of bupivacaine hydrochloride released in vitro. The results indicate that the designed in situ gelling systems are suitable for bupivacaine prolonged ophthalmic release and overcome the principal disadvantages of the liquid’s ocular formulations. An immediate therapeutic effect corresponding to ocular anesthetic installation was assured in the first stage: burst bupivacaine release. In the second phase, the gradual drug release was assured for over 6 h. This drug release profile, together with the corresponding rheological profile and a collection of superficial properties for good ocular adhesion balanced with an adequate hydrophilic character, assured the desired quality of the attributes for the proposed systems. The system, based on chitosan 1%, HPMC E 5 LV 5% and a 1/1 polymer ratio, could be a solution for the proposed formulation of in situ gelling colloidal systems, since the viscosity of the system was within the range of the optimal viscosity of the eye, and the amount of bupivacaine hydrochloride released after 6 h was the highest at 69.55%.

scholarly journals An Injectable and In Situ-Gelling Biopolymer for Sustained Drug Release Following Perineural Administration

Spine ◽  
2008 ◽  
Vol 33 (7) ◽  
pp. 748-754 ◽  
Author(s):  
Mohammed F. Shamji ◽  
Lyman Whitlatch ◽  
Allan H. Friedman ◽  
William J. Richardson ◽  
Ashutosh Chilkoti ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Drug Release ◽  
In Situ Gelling

DESIGN, CHARACTERIZATION AND EVALUATION OF MUCOADHESIVE NASAL IN SITU GELLING FORMULATIONS OF VENLAFAXINE HYDROCHLORIDE FOR BRAIN TARGETTING

INDIAN DRUGS ◽  
2016 ◽  
Vol 53 (01) ◽  
pp. 25-31
Author(s):  
M Priyanka ◽  
◽  
F. S. Dasankoppa ◽  
H. N Sholapur ◽  
NGN Swamy ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Linear Regression Analysis ◽  
Entrapment Efficiency ◽  
Stability Study ◽  
Drug Content ◽  
Venlafaxine Hydrochloride ◽  
In Situ Gelling

The poor bioavailability and the therapeutic effectiveness exhibited by the anti-depressant venlafaxine hydrochloride on oral administration is overcome by the use of ion-activated gel forming systems that are instilled as drops; these undergo gelation in the nasal cavity. The present study describes the design, characterization and evaluation of mucoadhesive nasal in situ gelling drug delivery of venlafaxine hydrochloride using different polymers like sodium alginate, HPMC and pectin in various concentrations. DSC studies revealed compatibility of the drug and excipients used. The in situ gels were characterized for physicochemical parameters, gelling ability, rheological studies, drug content, drug entrapment efficiency, in vitro mucoadhesive strength, water holding capacity, gel expansion coefficient and in vitro drug release studies. The amount of polymer blends was optimized using 23 full factorial design. The influence of experimental factors on percentage cumulative drug release at the end of 2 and 8 hours were investigated to get optimized formulation. The responses were analyzed using ANOVA and polynomial equation was generated for each response using multiple linear regression analysis. Optimized formulation, F9, containing 1.98% w/V sodium alginate, 0.64% w/V hydroxylpropyl methylcellulose, 0.99% w/V pectin showed percentage cumulative drug release of 19.33 and 80.44 at the end of 2 and 8 hours, respectively, which were close to the predicted values. The optimized formulation was subjected to stability study for three months at 300C /75% RH. The stability study revealed no significant change in pH, drug content and viscosity. Thus, venlafaxine hydrochloride nasal mucoadhesive in situ gel could be successfully formulated to improve bioavailability and to target the brain.

scholarly journals Formulation and characterization of a novel pH-triggered in-situ gelling ocular system containing Gatifloxacin

1970 ◽  
Vol 1 (3) ◽  
pp. 43-49 ◽  
Author(s):  
Jovita Kanoujia ◽  
Kanchan Sonker ◽  
Manisha Pandey ◽  
Koshy M Kymonil ◽  
Shubhini A Saraf
Keyword(s):  
Drug Release ◽  
Research Work ◽  
Gelling Agent ◽  
In Vitro Drug Release ◽  
Drug Content ◽  
Carbopol 940 ◽  
In Situ Gelling ◽  
Gel Transition

The present research work deals with the formulation and evaluation of in-situ gelling system based on sol-to-gel transition for ophthalmic delivery of an antibacterial agent gatifloxacin, to overcome the problems of poor bioavailability and therapeutic response exhibited by conventional formulations based a sol-to-gel transition in the cul-de-sac upon instillation. Carbopol 940 was used as the gelling agent in combination with HPMC and HPMC K15M which acted as a viscosity enhancing agent. The prepared formulations were evaluated for pH, clarity, drug content, gelling capacity, bioadhesive strength and in-vitro drug release. In-vitro drug release data of optimized formulation (F12) was treated according to Zero, First, Korsmeyer Peppas and Higuchi kinetics to access the mechanism of drug release. The clarity, pH, viscosity and drug content of the developed formulations were found in range 6.0-6.8, 10-570cps, 82-98% respectively. The gel provided sustained drug release over an 8 hour period. The developed formulation can be used as an in-situ gelling vehicle to enhance ocular bioavailability and the reduction in the frequency of instillation thereby resulting in better patient compliance. Key Words: In-situ gelation; Gatifloxacin; Carbopol 940; HPMC K15M. DOI: http://dx.doi.org/10.3329/icpj.v1i3.9661 International Current Pharmaceutical Journal 2012, 1(3): 43-49

scholarly journals DESIGN, DEVELOPMENT, AND EVALUATION OF AN ION-ACTIVATED OPHTHALMIC IN SITU GEL OF MOXIFLOXACIN HYDROCHLORIDE

2019 ◽  
pp. 94-103
Author(s):  
GIRISH KONDALKAR ◽  
ASISH DEV
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Statistical Models ◽  
Bacterial Infections ◽  
Gelling Agent ◽  
Design Development ◽  
Sustained Drug Release ◽  
Exchange Method ◽  
In Situ Gelling

Objective: The objective of this study was to develop an in situ ophthalmic gel of an anti-infective drug, moxifloxacin (MOX) hydrochloride (HCL), for sustained ocular delivery for the treatment of bacterial infections of the eye. Method: In the present work the in situ gelling systems were prepared by ion exchange method with the help of various concentrations of gelling agent gelrite (0.08 g, 0.1 g and 0.12 g) and sodium alginate (0.6 g, 0.8 g and 1 g) as viscosity enhancer were added in the formulation; 9 formulations were prepared according to 32 factorial designs and evaluated. The responses were analyzed for the analysis of variance using Design-Expert version 10 software. Statistical models were generated for each response parameter. Results: Optimized formulation batch F7 (0.12% gelrite and 0.6% sodium alginate) was liquid before addition of simulated tear fluid (STF) and underwent rapid gelation on addition of STF and had given 84.05% cumulative drug release; the formulation was found to be clear, having good in situ gelling capacity, good antibacterial efficacy, having drug content 99.75%; optimized formulation was sterile and showed sustained drug release over 8 h period as compared to marketed eye drop. Conclusions: From the above results, we can concluded that 32 full factorial design and statistical models can be successfully used to optimize the formulations, and it was concluded that the trial batch F7 (0.12% gelrite and 0.6% sodium alginate) is the best formula (percentage cumulative drug release over 84.05%) and it is possible to formulate in situ ophthalmic gels of MOX HCL using gelrite in combination with sodium alginate for the treatment of various bacterial infections of the eyes.

scholarly journals Tuning HIV drug release from a nanogel-basedin situforming implant by changing nanogel size

2019 ◽  
Vol 7 (3) ◽  
pp. 373-383 ◽  
Author(s):  
Adam R. Town ◽  
Jessica Taylor ◽  
Karl Dawson ◽  
Edyta Niezabitowska ◽  
Nancy M. Elbaz ◽  
...  
Keyword(s):  
Drug Release ◽  
Long Acting

This paper reports anin situforming implant based on responsive nanogels that gives tuneable long-acting drug release.

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

Systematic Development and Optimization of an in-situ Gelling System for Moxifloxacin Ocular Nanosuspension using High-pressure Homogenization with an Improved Encapsulation Efficiency

2018 ◽  
Vol 24 (13) ◽  
pp. 1434-1445 ◽  
Author(s):  
Lalit Kumar Khurana ◽  
Romi Singh ◽  
Harinder Singh ◽  
Manju Sharma
Keyword(s):  
High Pressure ◽  
Process Parameters ◽  
Encapsulation Efficiency ◽  
Quality By Design ◽  
Polynomial Equation ◽  
Single Type ◽  
Application Site ◽  
High Pressure Homogenization ◽  
In Situ Gelling

Background: The objective of this study was to apply Quality by Design (QbD) principles on process parameter optimization for the development of hybrid delivery system (combination of (SLNs) and In-situ gelling system) for hydrophilic drug Moxifloxacin Hydrochloride (MOX) to achieve its controlled delivery, which otherwise may not be possible through single type of technology. Methods: Risk assessment studies were carried out to identify probable risks influencing CQAs on the product. In design of experiments (DoE), the process parameters (independent variables) i.e., chiller temperature X1, High Pressure Homogenization (HPH) pressure X2, and HPH cycles X3 were optimized using a three-factor two level face-centered central composite design to streamline the influence on three responses, namely encapsulation efficiency Y1, particle size Y2 and outlet temperature Y3. Independent and dependent variables were analyzed to establish a full-model second-order polynomial equation. F value is used to confirm the omission of insignificant parameters/interactions to derive a reduced-model polynomial equation to predict the Y1, Y2 and Y3 for optimized moxifloxacin in situ gelled nanosuspension. Results: Desirability plots showed the effects of X1, X2, and X3 on Y1, Y2 and Y3, respectively. The design space is generated to obtain optimized process parameters viz. chiller temperature (-5°C), HPH pressure 800 – 900 bar and 8 cycles that resulted in nanosuspension with ≈ 500 nm size, encapsulation efficiency >65% and final formulation temperature <23°C that were necessary to maintain the formulation in a liquid state. Conclusion: Quality by Design (QbD) approach is recently been encouraged by regulatory bodies to improve the quality of the finished product. This approach proved to be a useful tool in the development of robust nanosuspension of highly hydrophilic drugs with improved efficiency. Results indicate that such hybrid gel systems can be used to control the release of SLNs from application site and prolong their action in a sustained manner.

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