Improved Skin Delivery of Voriconazole with a Nanostructured Lipid Carrier-Based Hydrogel Formulation

The aim of this study was to investigate the ability of NLC in increasing photostability of tomato extract in term of antioxidant activity. Photostability testing on antioxidant activity of samples were conducted by accelerating method using UVB radiation 32.400 joule for 21 hours radiation. Antioxidant activity was measured by DPPH method. NLC was made by High Shear Homogenization (HPH) method at 24000 rpm for 4 cycles, while conventional creame was made by low speed at 400 rpm. The product were characterized include: pH, viscosity, and particle size. There were had difference characters and physical stability. NLC had smaller size, more homogenous and more stable than conventional creame. It was known that stability of antioxidant activity of tomato extract in NLC system higher than in conventional creame. That was showed with k value, as constanta of rate scavenging activity decreasing in antioxidant power between time (Sigma 2-tail less than 0.005) of NLC and conventional creame were: 2.03x10-2 %/hour ±0.08 (3.94) and 4.71x 10-2 %/ hour ±0.23 (4.88) respectively.

Download Full-text

Nano-Sized Technologies for Miconazole Skin Delivery

Current Pharmaceutical Biotechnology ◽

10.2174/1389201017666160301102459 ◽

2016 ◽

Vol 17 (6) ◽

pp. 524-531 ◽

Cited By ~ 11

Author(s):

Alireza Firooz ◽

Roshanak Namdar ◽

Shohreh Nafisi ◽

Howard I. Maibach

Keyword(s):

Skin Delivery

Download Full-text

Improving Topical Skin Delivery of Monocrotaline Via Liposome Gel-based Nanosystems

Current Drug Delivery ◽

10.2174/1567201816666191029125300 ◽

2019 ◽

Vol 16 (10) ◽

pp. 940-950 ◽

Cited By ~ 1

Author(s):

Jiandong Yu ◽

Zhi Chen ◽

Yan-zhi Yin ◽

Chaoyuan Tang ◽

Enying Hu ◽

...

Keyword(s):

Gradient Method ◽

Encapsulation Efficiency ◽

Ph Value ◽

Topical Administration ◽

Ph Gradient ◽

Stability Factor ◽

Buffer Solution ◽

Skin Delivery ◽

Skin Retention

Background: In this study, a liposomal gel based on a pH-gradient method was used to increase the skin-layer retention of monocrotaline (MCT) for topical administration. Methods: Using the Box-Behnken design, different formulations were designed to form liposome suspensions with optimal encapsulation efficiency (EE%) and stability factor (KE). In order to keep MCT in liposomes and accumulate in skin slowly and selectively, MCT liposome suspensions were engineered into gels. Results: A pH-gradient method was used to prepare liposome suspensions. The optimal formulation of liposome suspensions (encapsulation efficiency: 83.10 ± 0.21%) was as follows: MCT 12 mg, soybean phosphatidyl choline (sbPC) 200 mg, cholesterol (CH) 41 mg, vitamin E (VE) 5 mg, and citric acid buffer solution (CBS) 4.0 10 mL (pH 7.0). The final formulation of liposomal gels consisted of 32 mL liposome suspensions, 4.76 mL deionized water, 0.40 g Carbopol-940, 1.6 g glycerol, 0.04 g methylparaben, and a suitable amount of triethanolamine for pH value adjustment. The results of in vitro drug release showed that MCT in liposomal gels could be released in 12 h constantly in physiological saline as a Ritger-Peppas model. Compared with plain MCT in gel form, liposomal MCT in gel had higher skin retention in vitro. Conclusion: In this study, liposomal gels were formed for greater skin retention of MCT. It is potentially beneficial for reducing toxicities of MCT by topical administration with liposomal gel.

Download Full-text

Design and Synthesis of a Novel Gabapentin-Phosphotidylcholine Conjugate for Targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier

Current Computer - Aided Drug Design ◽

10.2174/1573409916666201224153414 ◽

2020 ◽

Vol 16 ◽

Author(s):

Anjali P.B ◽

Jawahar N. ◽

Jubie S. ◽

Neetu Yadav ◽

Selvaraj A. ◽

...

Keyword(s):

Drug Release ◽

Phospholipase A2 ◽

Release Kinetics ◽

Entrapment Efficiency ◽

Structural Analog ◽

Fickian Diffusion ◽

Release Kinetic ◽

Nanostructured Lipid Carrier ◽

Discovery Studio

Background: : Epilepsy is a genuine neurological turmoil that effects around 50 million individuals around the world. Practically 30% of epileptic patients experience the ill effects of pharmaco-obstruction, which is related with social seclusion, subordinate conduct, low marriage rates, joblessness, mental issues and diminished personal satisfaction. At present accessible antiepileptic drugs have a restricted viability, and their negative properties limit their utilization and cause challenges in patient administration. Gabapentin 1-(aminomethyl)cyclohexane acetic acid, Gbp , (trade name Neurontin), a structural analog of γ-aminobutyric acid (GABA), BCS class 3 drug with having permeability issues. Objective: This work was an attempt to formulate and characterize a new approach to treat epilepsy by targeting to Phospholipase A2 Enzyme through Nanostructured Lipid Carrier. Methods: Docking studied carried out using Accelrys Discovery studio 4.1 Client and gabapentin and phosphotidylcholine were conjugated through chemical conjugation. Nanostructured lipid carrier (NLC) was prepared using hot homogenization technique. Results: The libdock score of Gabapentin- Phosphotidylcholine conjugate (192.535) were found to be more than Gabapentin (77.1084) and Phosphotidylcholine (150.212). For the optimized formulation the particle size (50.08), zeta potential (-1.48), PDI (0.472) and entrapment efficiency (77.8) was observed. The NLC was studies for in-vitro drug release studies and release kinetics. Finally found that the drug release from the NLC followed Higuchi release kinetic and the mode of drug release from the NLC was found to be Non- Fickian diffusion. Conclusion: The formulated Nanostructured lipid carrier of Gabapentin-Phosphotidylcholine conjugate may be able to use to prevent seizure.

Download Full-text

Formulation Development of Tamoxifen Loaded Lipid Nanoparticle by Taguchi (L12 (2 11)) Orthogonal Array Design

Current Computer - Aided Drug Design ◽

10.2174/1573409916666200320162948 ◽

2020 ◽

Vol 16 ◽

Author(s):

Poovi Ganesan ◽

N Damodharan

Keyword(s):

Orthogonal Array ◽

Drug Loading ◽

Optimization Technique ◽

Pharmaceutical Products ◽

Water Soluble ◽

Nanostructured Lipid Carrier ◽

Orthogonal Array Design ◽

Formulation Development ◽

Array Design ◽

Lipid Nanoparticle

Background: A better understanding of the biopharmaceutical and physicochemical properties of drugs and the pharmaco-technical factors would be of great help for developing pharmaceutical products. But, it is extremely difficult to study the effect of each variable and interaction among them through the conventional approach Objective: To screen the most influential factors affecting the particle size (PS) of lipid nanoparticle (LNPs) (solid lipid nanoparticle (SLN) and nanostructured lipid carrier (NLC)) for poorly water-soluble BCS class-II drug like tamoxifen (TMX) to improve its oral bioavailability and to reduce its toxicity to tolerable limits using Taguchi (L12 (2 11)) orthogonal array design by applying computer optimization technique. Results: The size of all LNPs formulations prepared as per the experimental design varied between 172 nm and 3880 μm, polydispersity index between 0.033 and 1.00, encapsulation efficiency between 70.8% and 75.7%, and drug loading between 5.84% and 9.68%. The study showed spherical and non-spherical as well as aggregated and non-aggregated LNPs. Besides, it showed no interaction and amorphous form of the drug in LNPs formulation. The Blank NLCs exhibited no cytotoxicity on MCF-7 cells as compared to TMX solution, SLNs (F5) and NLCs (F12) suggests that the cause of cell death is primarily from the effect of TMX present in NLCs. Conclusions: The screening study clearly showed the importance of different individual factors significant effect for the LNPs formulation development and its overall performance in an in-vitro study with minimum experimentation thus saving considerable time, efforts, and resources for further in-depth study.

Download Full-text

Cancer Nanotechnology-An Excursion on Drug Delivery Systems

Anti-Cancer Agents in Medicinal Chemistry ◽

10.2174/1871520618666180720164015 ◽

2019 ◽

Vol 18 (15) ◽

pp. 2078-2092 ◽

Cited By ~ 2

Author(s):

Mala Sharma ◽

Chitranshu Pandey ◽

Neha Sharma ◽

Mohammad A. Kamal ◽

Usman Sayeed ◽

...

Keyword(s):

Drug Delivery ◽

Targeted Delivery ◽

Drug Delivery Systems ◽

Cancer Chemoprevention ◽

Delivery Systems ◽

Nanostructured Lipid Carrier ◽

Nanodrug Delivery ◽

Drug Conjugates ◽

Drug Nanoparticles ◽

Cancer Nanotechnology

Background: Nanotechnology pictures a breakthrough in the domain of cancer therapy owing to its novel properties and functions. This technology is quite amendable as it allows the scientists to engineer drug nanoparticles of dimensions 10nm – 500nm permitting them to pass via leaky vasculature of tumorigenic microenvironment with higher specificity, reduced cytotoxicity and effective release without any after effects. The central part of the review zooms onto the role of nanoparticles and their targeted delivery for the cure of cancer. Methods: The novel and various versatile nanoparticle platforms viz. polymeric (drug-conjugates, micelles, dendrimers), Lipid-based (liposomes, solid nanoparticle, nanostructured lipid carrier, lipid-polymer hybrid), and stimuli-sensitive (thermoresponsive, ultrasound, pH-responsive, hydrogel) etc. have been designed for a persistent, précised nanodrug delivery and the co-delivery of collegial drug conjugates leading to the formation of safer release of myriad of drugs for cancer chemoprevention. Results: The review concerns about tracing and detailing the drug delivery systems of cancer nanotechnology. Conclusion: Nanotechnology is bestowed with the design, depiction, fabrication, and application of nanostructures, and devices with their controlled delivery together with the imaging of the selected target site and drug release at the specific site of action.

Download Full-text

FORMULATION AND IN VITRO, IN VIVO EVALUATION OF PRONIOSOMAL GEL OF NEOMYCIN SULPHATE

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i2.30614 ◽

2019 ◽

pp. 156-163

Author(s):

AMOL SHETE ◽

PRIYANKA THORAT ◽

RAJENDRA DOIJAD ◽

SACHIN SAJANE

Keyword(s):

Phase Separation ◽

Skin Irritation ◽

Entrapment Efficiency ◽

Separation Method ◽

Gelling Agent ◽

In Vivo Evaluation ◽

Skin Delivery ◽

Span 60

Objective: The objectives of present investigation were to prepare and evaluate proniosomes of neomycin sulphate (NS) by coacervation phase separation method by using sorbitan monostearate (span 60) and lecithin as a surfactant to increase the penetration through the skin and study the effect of concentration of the same. Methods: Proniosomes of neomycin sulphate (NS) were prepared by coacervation phase separation method by using span 60 and lecithin. The effect of concentration of span 60 and lecithin was studied by factorial design. The prepared proniosomes were converted to gel by using carbopol as a gelling agent. The prepared formulations were evaluated for entrapment efficiency, in vitro drug diffusion, in vitro antibacterial activity and in vivo skin irritation test etc. Results: All Formulation showed the percentage entrapment efficiency in the range 38.31±0.05% to 77.96±0.06%, good homogeneity and gel was easily spreadable with minimal of shear. Optimized formulation showed enhanced rate of diffusion in vitro, increase in zone of inhibition against staphylococcus aureus, no skin irritation and showed good stability. Conclusion: The results of present study indicates that proniosomal gel formulated by using combination of span 60, Lecithin, cholesterol can be used to enhance skin delivery of NS because of excellent permeation of drug. Developed proniosomal gel formulation was promising carrier for NS

Download Full-text

Dexamethasone-Loaded Nanostructured Lipid Carriers for the Treatment of Dry Eye Disease

Pharmaceutics ◽

10.3390/pharmaceutics13060905 ◽

2021 ◽

Vol 13 (6) ◽

pp. 905

Author(s):

Sangeeta Kumari ◽

Madhuri Dandamudi ◽

Sweta Rani ◽

Elke Behaeghel ◽

Gautam Behl ◽

...

Keyword(s):

Dry Eye ◽

Ocular Surface ◽

Pilot Scale ◽

Dry Eye Disease ◽

Rapid Screening ◽

Eye Disease ◽

Topical Steroids ◽

Nanostructured Lipid Carrier ◽

The Impact ◽

Ophthalmic Formulation

Dry eye disease (DED) or keratoconjunctivitis sicca is a chronic multifactorial disorder of the ocular surface caused by tear film dysfunction. Symptoms include dryness, irritation, discomfort and visual disturbance, and standard treatment includes the use of lubricants and topical steroids. Secondary inflammation plays a prominent role in the development and propagation of this debilitating condition. To address this we have investigated the pilot scale development of an innovative drug delivery system using a dexamethasone-encapsulated cholesterol-Labrafac™ lipophile nanostructured lipid carrier (NLC)-based ophthalmic formulation, which could be developed as an eye drop to treat DED and any associated acute exacerbations. After rapid screening of a range of laboratory scale pre-formulations, the chosen formulation was prepared at pilot scale with a particle size of 19.51 ± 0.5 nm, an encapsulation efficiency of 99.6 ± 0.5%, a PDI of 0.08, and an extended stability of 6 months at 4 °C. This potential ophthalmic formulation was observed to have high tolerability and internalization capacity for human corneal epithelial cells, with similar behavior demonstrated on ex vivo porcine cornea studies, suggesting suitable distribution on the ocular surface. Further, ELISA was used to study the impact of the pilot scale formulation on a range of inflammatory biomarkers. The most successful dexamethasone-loaded NLC showed a 5-fold reduction of TNF-α production over dexamethasone solution alone, with comparable results for MMP-9 and IL-6. The ease of formulation, scalability, performance and biomarker assays suggest that this NLC formulation could be a viable option for the topical treatment of DED.

Download Full-text