scholarly journals In vitro kinetic release study, antimicrobial activity and in vivo toxicity profile of a kojic acid ester-based nanoemulsion for topical application

RSC Advances ◽  
2020 ◽  
Vol 10 (71) ◽  
pp. 43894-43903
Author(s):  
Sharifah Nurfadhlin Afifah Syed Azhar ◽  
Siti Efliza Ashari ◽  
Syahida Ahmad ◽  
Norazlinaliza Salim

Nanoemulsions have emerged as novel vehicles for drug delivery that allow sustained or controlled release for topical application.

MRS Bulletin ◽  
2004 ◽  
Vol 29 (1) ◽  
pp. 33-37 ◽  
Author(s):  
Waltraud M. Kriven ◽  
Seo-Young Kwak ◽  
Matthew A. Wallig ◽  
Jin-Ho Choy

AbstractNanoscale ceramic particles, such as layered double hydroxides (LDHs), have been developed to deliver drugs or genes into biological cells. In this article, we describe the controlled-release properties of LDHs as drug delivery carriers, the formation of bio-LDH nanohybrids, theirin vivoandin vitrocytotoxicity tests, and their potential as anticancer gene delivery carriers. Unstable biomolecules can be intercalated into LDHs, displacing the interlayer anions; the drug or gene's negative charge is thus shielded, enabling penetration into the cell. In the slightly acidic environment of the cell, ceramic nanoplatelets of ∼100 nm diameter dissolve, thus releasing the intercalates in a controlled manner.


2020 ◽  
Vol 17 ◽  
Author(s):  
Bhaskar Kurangi ◽  
Sunil Jalalpure ◽  
Satveer Jagwani

Aim: The aim of the study was to formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC) through topical application. Background: Resveratrol (RV) is a nutraceutical compound that has exciting pharmacological potential in different diseases including cancers. Many studies of resveratrol have been reported for anti-melanoma activity. Due to its low bioavailability, the activities of resveratrol are strongly limited. Hence, an approach with nanotechnology has been done to increase its activity through transdermal drug delivery. Objective: To formulate, characterize, and evaluate the resveratrol-loaded cubosomes (RC). To evaluate resveratrol-loaded cubosomal gel (RC-Gel) for its topical application. Methods: RC was formulated by homogenization technique and optimized using a 2-factor 3-level factorial design. Formulated RCs were characterized for particle size, zeta potential, and entrapment efficiency. Optimized RC was evaluated for in vitro release and stability study. Optimized RC was further formulated into cubosomal gel (RC-Gel) using carbopol and evaluated for drug permeation and deposition. Furthermore, developed RC-Gel was evaluated for its topical application using skin irritancy, toxicity, and in vivo local bioavailability studies. Results: The optimized RC indicated cubic-shaped structure with mean particle size, entrapment efficiency, and zeta potential were 113±2.36 nm, 85.07 ± 0.91%, and -27.40 ± 1.40 mV respectively. In vitro drug release of optimized RC demonstrated biphasic drug release with the diffusion-controlled release of resveratrol (RV) (87.20 ± 2.25%). The RC-Gel demonstrated better drug permeation and deposition in mice skin layers. The composition of RC-Gel has been proved non-irritant to the mice skin. In vivo local bioavailability study depicted the good potential of RC-Gel for skin localization. Conclusion: The RC nanoformulation proposes a promising drug delivery system for melanoma treatment simply through topical application.


PLoS ONE ◽  
2014 ◽  
Vol 9 (12) ◽  
pp. e115952 ◽  
Author(s):  
Jaganmohan Somagoni ◽  
Cedar H. A. Boakye ◽  
Chandraiah Godugu ◽  
Apurva R. Patel ◽  
Henrique Antonio Mendonca Faria ◽  
...  

2014 ◽  
Vol 2 (48) ◽  
pp. 8616-8625 ◽  
Author(s):  
Peilin Huang ◽  
Jingnan Wang ◽  
Shuting Lai ◽  
Fang Liu ◽  
Nan Ni ◽  
...  

Drug delivery nanosystems have been designed as Enro-NH2-TNTs and Enro-SH-TNTs with high bioactivity and excellent in vitro and in vivo controlled release.


2021 ◽  
Vol 28 ◽  
Author(s):  
Diego Arauna ◽  
Sekar Vijayakumar ◽  
Esteban Durán-Lara

Background: Drug delivery systems such as hydrogels have become relevant in cardiovascular and metabolic therapies due to their sustained and controlled release properties of drugs, versatile polymer structures, safety and biodegradability. Results: The literature presented demonstrates that a hydrogel-based controlled release system increases the therapeutic efficacy in different components of the metabolic syndrome. Hypertension has been the most explored component with advances in vitro and murine models. However, clinical evidence in humans is scarce, and more translational studies are needed. Hydrogel-based systems for diabetes, obesity, and dyslipidemia have been little explored. Observations mainly demonstrated an increase in therapeutic efficacy, in vitro and in vivo, for the use of insulin, leptin, and natural components, such as epigallocatechin gallate. In all cases, the hydrogel systems achieve better plasma levels of the loaded compound, higher bioavailability, and low cytotoxicity; compared to conventional systems. Also, the evidence existing suggests that the development of an injectable hydrogel system for controlled release of drugs or therapeutic compounds is presented as an attractive option for MeS treatment, due to the possibility of sustained pharmacological release, no need for repeated doses, and a safe administration route. Conclusion: The following review aims to evaluate the use of the hydrogel systems in the therapy of diabetes, obesity, hypertension, and dyslipidemia, which are the main components of metabolic syndrome.


Author(s):  
Rajesh Pawar ◽  
Swati Jagdale

Aim: This research work was aimed to evaluate Metformin hydrochloride (MH) floating dosage form by In vitro evaluation/In vivo prediction and to evaluate it’s predictability through it’s application during the R&D using Insilico technique in WINONLIN Software. MH was examined as a model drug, which is a biguanide and is an hypoglycemic agent administered orally. The study was aimed to determine the the systemic concentrations of MH using In-vivo prediction. Study Design: Fabrication and assessment of Metformin hydrochloride floating drug delivery system: In Vitro evaluation /In Vivo prediction. Biorelevant media was selected for dissolution profile of 12 units of dosage form. Software assisted program used for data feeding and results output. Methodology: The absorption window for MH is the upper portion of the small gut in which the GI absorption is complete after 6 h. Hence gastroretentive formulation was developed and validity of dissolution study was extended by In vivo pharmacokinetic prediction using WinNonlin Software. A mechanistic oral absorption model was built in Phoenix WinNonlin® software. In the presented work, significant yet crucial, gastrointestinal (GI) variables are considered for biopredictive dissolution testing to account for a valuable input for physiologically-based pharmacokinetic (PBPK) platform programs. While simulations are performed and mechanistic insights are gained from such simulations from the WinNonlin program. Results: These floating tablets were observed for In vitro release and studied for In vivo pharmacokinetic prediction. From the obtained values, a meaningful In vivo prediction was done. interestingly from the results attained floating tablets showed sustained drug release and extended drug absorbed in 24h. Fascinatingly, from the data it was proved that drug formulation resides for desired time. The absorption of MH from the developed CR tablet was 1.4 fold higher than its marketed tablet and it had higher AUC0–t values than the marketed product which indicates superior bioavailability of test product compared to marketed tablet with similar dose in Invivo pharmacokinetic prediction. The mean value of biological half-life (t1/2) and Tmax of MH from test formulation is two times more, Test product has shown higher MRT, showing that the drug is maintained longer in the body in comparison to marketed product indicates controlled absorption. Conclusion: Here we concluded that, a comparative prediction pharmacokinetic evaluation of the fabricated controlled release tablets and the marketed formulation indicates that the fabricated controlled release tablets are well absorbed and the degree of absorption is greater than that of the marketed ER formulation with larger gastric residence time.


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