scholarly journals Solid Lipid Microparticles Loaded Hydrogel Formulation for Transdermal Delivery of Glucosamine Sulphate

2021 ◽  
Vol 10 (14) ◽  
pp. 1030-1034
Author(s):  
Sundareswara Kumar Chellaswamy ◽  
Satheesh Babu Natrajan
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Encapsulation Efficiency ◽  
Stability Studies ◽  
Potential Value ◽  
Solid Lipid ◽  
Age Related ◽  
Dispersion Technique

BACKGROUND Osteoarthritis is a common, age-related, chronic and slowly progressive joint disorder which ultimately leads to joint failure. To achieve sustained release drug delivery and ease of administration, the present study was carried out to formulate a glucosamine solid lipid microparticle-based hydrogel. METHODS 20 batches of glucosamine solid lipid microparticle were prepared by melt dispersion technique. They were then evaluated with regard to various parameters such as physical appearance, pH analysis, spreadability, viscosity, drug content, in vitro drug release and accelerated stability studies. Then the glucosamine solid lipid microparticle-based hydrogel was compared with the glucosamine loaded hydrogel. RESULTS Of these batches, batches 18, 19 and 20 of increasing homogenizing speed of 1000, 1500 and 2000 rpm were found be efficient but the batch 18 showed better encapsulation efficiency. Batch 18 showed particle size of 86 ± 5 µm, encapsulation efficiency of 81.74 ± 4.5 and the zeta potential value of - 29 ± 1. So, batch 18 was found to be the optimised formulation which was further taken for incorporating the Carbopol. The efficient encapsulated glucosamine solid lipid microparticle-based hydrogel was formulated. There were no significant changes in physicochemical properties on stability studies. CONCLUSIONS Glucosamine solid lipid microparticle-based hydrogel had good particle size, high encapsulation efficiency and high zeta potential value and showed high percentage drug release which was better than the glucosamine loaded hydrogel. KEY WORDS Glucosamine Solid Lipid Microparticle Based Hydrogel, Osteoarthritis, Encapsulation Efficiency, Zeta Potential, Melt Dispersion Technique

scholarly journals FORMULATION AND EVALUATION OF CURCUMIN LOADED LIPOSOME AND ITS BIO-ENHANCEMENT

2019 ◽  
Vol 9 (4-A) ◽  
pp. 425-437
Author(s):  
Khushboo Verma ◽  
Jhakeshwar Prasad ◽  
Suman Saha ◽  
Surabhi Sahu
Keyword(s):  
Thin Film ◽  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
High Performance ◽  
Encapsulation Efficiency ◽  
Mean Particle Size ◽  
Liposome Formulation

The aim of this work was to develop and evaluate curcumin loaded liposome and its bio- enhancement. Curcumin was selected as a natural drug for liposome formulation. Curcumin show variety of biological activity but it also shows poor bioavailability due to low aqueous solubility (1 µg/ml), poor absorption and rapid metabolism so that piperine was selected as bio enhancer to improve curcumin bioavailability. Soy lecithin and cholesterol were used to prepared curcumin and curcumin-piperine loaded liposome at different ratio by thin film hydration method because of easy to perform, and high encapsulation rates of lipid. The all liposome formulations (F1-F5) were evaluated by mean particle size, polydispersity index, zeta potential, encapsulation efficiency and drug release. Bioavailability was also determined on rat. Blood samples were collected at specific intervals, and plasma was separated by ultracentrifugation. Plasma was analyzed by high-performance liquid chromatography at 425 nm taking acetonitrile: water (75:25 v/v) acidified with 2% acetic acid as a mobile phase at a flow rate of 0.5 ml/min using C18 column. The mean particle size was found in the range between 800-1100 that indicate liposome are large unilamellar vesical types. By zeta potential study its conform that the all formulation was stable. The encapsulation efficiency of all liposome formulation are varied between 59-67%. In vitro drug release was analyse in 7.4 pH phosphate buffer, the maximum %CDR observed at the 12 hrs., and formulation are follow sustained release thus they reduce metabolism, good absorption rate which improve bioavailability of drug. From in-vivo study, it is clear that curcumin-piperine liposomal formulation, increases Cmax, area under the curve, and mean residence time significantly as compared to pure curcumin and pure curcumin liposome. Keywords: liposome; Curcumin; Piperine, Thin film hydration method; Bioavailability

scholarly journals Design, Development and Evaluation Of Anti-Hypertensive Drug Solid Lipid Nano Particles

2021 ◽  
Vol 11 (4) ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Entrapment Efficiency ◽  
Nano Particles ◽  
Release Mechanism ◽  
In Vitro Drug Release ◽  
Solid Lipid ◽  
Wide Range

Recently, solid lipid Nano-particles have received much attention by the researchers owing to its biodegradability, biocompatibility and the ability to deliver a wide range of drugs. The aim of the present study was to design Diltiazem solid lipid Nano-particles and to evaluate them. Diltiazem solid lipid Nano-particles were prepared by hot homogenization technique using different lipids (Tristearin, GMS and Comprital), soy lecithin as stabilizers and tween 80, Poloxamer as surfactants. The Nano-particles were evaluated for particle size & PDI, zeta potential, entrapment efficiency and in vitro drug release. The particle size ranged from 49.7 to 523.7 nm. PDI of all formulations were good within the range of 0.189 to 0.427. The zeta potential ranged from -10.5 to -29.6 Mv, Entrapment efficiency of all formulations were observed was in the range of 78.68 to 95.23 %. The cumulative percentage release of Diltiazem from different Diltiazem Nano-particles varied from 53.36 to 88.74% depending upon the drug lipid ratio and the type of lipid used. The average percentage of drug released from different SLNs after 24 hours showed in the following order: F9 (53.35%) < F6 (56.75%) < F4 (61.74%) < F7 (63.8%) < F5(67.77%) < F8(69.04%) < F3(75.31%) < F1(79.36%) <F2 (88.74%) respectively. The release kinetic studies showed that the release was first order diffusion controlled and the n values obtained from the Korsmeyer-Peppa’s model indicated the release mechanism was Quasi-Fickian type (n-value of 0.47). Keywords: Diltiazem, solid lipid Nano-particles, FTIR, in vitro drug release.

scholarly journals DEVELOPMENT, CHARACTERIZATION, AND EVALUATION OF SELEGILINE BIONANOSUSPENSIONS USING BUCHANANIA LANZAN AS BIOSTABILIZER

2019 ◽  
pp. 248-255
Author(s):  
YOGITA TYAGI ◽  
N. V. SATHEESH MADHAV
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Release Kinetics ◽  
Hydroxypropyl Methylcellulose ◽  
Polydispersity Index ◽  
Fickian Diffusion ◽  
Stability Studies ◽  
Best Fit

Objective: Development and evaluation of selegiline-loaded bio-nanosuspensions using biopolymer which was isolated from seeds of Buchanania lanzan (Chironji), used as biostabilizer and compared with standard polymer. Methods: The selegiline-loaded bio-nanosuspensions were prepared using novel biopolymer and standard stabilizer (hydroxypropyl methylcellulose) by sonication solvent evaporation method with different ratios (1%, 2%, 3%, 4%, and 5%) and evaluated for particle size, polydispersity index, zeta potential, pH stability studies, percentage entrapment efficacy, in vitro drug release, and stability studies. Results: The prepared selegiline bio-nanosuspensions were subjected to the best formulation based on comparison of above-mentioned evaluation parameters, so Fb2 (2%) formulation was found to be the best formulation showing an R2=0.9842, T50% of 32 h and T80% of 70 h, respectively. According to the release kinetics, the best fit model was found to be Peppas-Korsmeyer with Fickian diffusion (Higuchi matrix) as the mechanism of drug release, and Fs5 (5%) formulation was found to be the best formulation showing an R2=0.9564, T50% of 25 h and T80% of 60 h, respectively. According to the release kinetics, the best fit model was found to be Peppas-Korsmeyer with Fickian diffusion (Higuchi matrix) as the mechanism of drug release. The biopolymer provided excellent stability for the formulation and resulting particle size for the best formulation was found to be 360 nm. The best formulation was found to be polydispersity index of 0.43 with zeta potential of −5.12 mV. Conclusion: The prepared bio-nanosuspensions using biopolymer were found to be safe and compatible with the novel drug delivery for the treatment of depression in comparison of standard polymer.

scholarly journals Optimization and Characterization of Fenugreek Seed Polymer Nanoparticles Loaded with Diltiazem HCl Nanoparticles by Desolvation Method

2019 ◽  
Vol 9 (6-s) ◽  
pp. 155-163
Author(s):  
Munagala Gayatri Ramya ◽  
Rajesh Akki ◽  
Chakrala Jyothsna
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Surface Morphology ◽  
Encapsulation Efficiency ◽  
Polymer Concentration ◽  
Polymer Nanoparticles ◽  
Fenugreek Seed ◽  
Diltiazem Hcl

The main aim of the present investigation is to optimize and evaluate the fenugreek seed polymer nanoparticles using Diltiazem HCl as a model drug because Diltiazem HCl has short half-life. Nanoparticles were prepared by using desolvation method and evaluated to study the influence of polymer concentration and stirring speed on different characteristics of nanoparticles such as particle size, surface morphology, zeta potential, Encapsulation efficiency and In-vitro drug release. FTIR, DSC and XRD studies were also performed to determine the compatibility, degradation and crystalline nature of drug before and after formulation of nanoparticles. F7 (1:2 polymer concentration and 600 stirring speed) was optimized formulation based on its particle size (672.1nm), encapsulation efficiency (83.1) having higher stability of Zeta potential value of -26.2, smooth surface morphology and having higher retarded drug release with non fickkian diffusion. By studying all the characteristics it was finally concluded that a natural polymer obtained from fenugreek seed can be used as a rate controlling polymer in the preparation of nanoparticles. Keywords:  Diltiazem HCl, Fenugreek seed polymer, rate controlling polymer,      Nanoparticles, Desolvation.

Solid Lipid Nanoparticles for Topical Delivery of Acitretin for the Treatment of Psoriasis by Design of Experiment

2020 ◽  
Vol 12 (2) ◽  
pp. 4474-4491
Author(s):  
Rajkumar Aland ◽  
Ganesan M ◽  
P. Rajeswara Rao ◽  
Bhikshapathi D. V. R. N.
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Solid Lipid Nanoparticles ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Tem Analysis ◽  
In Vitro Drug Release ◽  
Solid Lipid

The main objective for this investigation is to develop and optimize the solid lipid nanoparticles formulation of acitretin for the effective drug delivery. Acitretin loaded SLNs were prepared by hot homogenization followed by the ultrasonication using Taguchi’s orthogonal array with eight parameters that could affect the particle size and entrapment efficiency. Based on the results from the analyses of the responses obtained from Taguchi design, three different independent variables including surfactant concentration (%), lipid to drug ratio (w/w) and sonication time (s) were selected for further investigation using central composite design. The  lipid Dynasan-116, surfactant poloxomer-188 and co surfactant egg lecithin resulted in better percent drug loading and evaluated for particle size, zeta potential, drug entrapment efficiency, in vitro drug release and stability. All parameters were found to be in an acceptable range. TEM analysis has demonstrated the presence of individual nanoparticles in spherical shape and the results were compatible with particle size measurements.  In vitro drug release of optimized SLN formulation (F2) was found to be 95.63 ± 1.52%, whereas pure drug release was 30.12 after 60 min and the major mechanism of drug release follows first order kinetics release data for optimized formulation (F2) with non-Fickian (anomalous) with a strong correlation coefficient (R2 = 0.94572) of Korsemeyer-Peppas model. The total drug content of acitretin gel formulation was found to 99.86 ± 0.012% and the diameter of gel formulation was 6.9 ± 0.021 cm and that of marketed gel was found to be 5.7 ± 0.06 cm, indicating better spreadability of SLN based gel formulation. The viscosity of gel formulation at 5 rpm was found to be 6.1 x 103 ± 0.4 x 103 cp. The release rate (flux) of acitretin across the membrane and excised skin differs significantly, which indicates about the barrier properties of skin. The flux value for SLN based gel formulation (182.754 ± 3.126 μg cm−2 h−1) was found to be higher than that for marketed gel (122.345 ± 4.786 μg cm−2 h−1). The higher flux and Kp values of SLN based gel suggest that it might be able to enter the skin easily as compared with marketed gel with an advantage of low interfacial tension of the emulsifier film that ensures an excellent contact to the skin. This topically oriented SLN based gel formulation could be useful in providing site-specific dermal treatment of psoriasis

Optimization and Characterization of Aqueous Micellar Formulations for Ocular Delivery of an Antifungal Drug, Posaconazole

2020 ◽  
Vol 26 (14) ◽  
pp. 1543-1555 ◽  
Author(s):  
Meltem E. Durgun ◽  
Emine Kahraman ◽  
Sevgi Güngör ◽  
Yıldız Özsoy
Keyword(s):  
Particle Size ◽  
Zeta Potential ◽  
Size Distribution ◽  
Encapsulation Efficiency ◽  
Fungal Infections ◽  
In Vitro Release ◽  
Pluronic F127 ◽  
Glycol Succinate ◽  
Vitro Release

Background: Topical therapy is preferred for the management of ocular fungal infections due to its superiorities which include overcoming potential systemic side effects risk of drugs, and targeting of drugs to the site of disease. However, the optimization of effective ocular formulations has always been a major challenge due to restrictions of ocular barriers and physiological conditions. Posaconazole, an antifungal and highly lipophilic agent with broad-spectrum, has been used topically as off-label in the treatment of ocular fungal infections due to its highly lipophilic character. Micellar carriers have the potential to improve the solubility of lipophilic drugs and, overcome ocular barriers. Objective: In the current study, it was aimed optimization of posaconazole loaded micellar formulations to improve aqueous solubility of posaconazole and to characterize the formulations and to investigate the physical stability of these formulations at room temperature (25°C, 60% RH), and accelerated stability (40°C, 75% RH) conditions. Method: Micelles were prepared using a thin-film hydration method. Pre-formulation studies were firstly performed to optimize polymer/surfactant type and to determine their concentration in the formulations. Then, particle size, size distribution, and zeta potential of the micellar formulations were measured by ZetaSizer Nano-ZS. The drug encapsulation efficiency of the micelles was quantified by HPLC. The morphology of the micelles was depicted by AFM. The stability of optimized micelles was evaluated in terms of particle size, size distribution, zeta potential, drug amount and pH for 180 days. In vitro release studies were performed using Franz diffusion cells. Results: Pre-formulation studies indicated that single D-ɑ-tocopheryl polyethylene glycol succinate (TPGS), a combination of it and Pluronic F127/Pluronic F68 are capable of formation of posaconazole loaded micelles at specific concentrations. Optimized micelles with high encapsulation efficiency were less than 20 nm, approximately neutral, stable, and in aspherical shape. Additionally, in vitro release data showed that the release of posaconazole from the micelles was higher than that of suspension. Conclusion: The results revealed that the optimized micellar formulation of posaconazole offers a potential approach for topical ocular administration.

scholarly journals Eluxadoline Loaded Solid Lipid Nanoparticles for Improved Colon Targeting in Rat Model of Ulcerative Colitis

2020 ◽  
Vol 13 (9) ◽  
pp. 255
Author(s):  
Md. Khalid Anwer ◽  
Mohammed Muqtader Ahmed ◽  
Mohammed F. Aldawsari ◽  
Saad Alshahrani ◽  
Farhat Fatima ◽  
...  
Keyword(s):  
Ulcerative Colitis ◽  
Acetic Acid ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
In Vitro Release ◽  
Lipid Nanoparticles ◽  
Stability Studies ◽  
Solid Lipid ◽  
Vitro Release

The aim of the current study was to evaluate the therapeutics potential of eluxadoline (ELX) loaded solid lipid nanoparticles (SLNs) in ulcerative colitis. ELX loaded SLNs were prepared using three different lipids according to the solvent emulsification technique. The optimization of prepared SLNs (F1-F3) were carried out based on size, PDI, zeta potential, percent drug entrapment (%EE), and loading (%DL). The lipid (stearic acid) based SLNs (F2) was optimized with particle size (266.0 ± 6.4 nm), PDI (0.217 ± 0.04), zeta potential (31.2 ± 5.19 mV), EE (65.0 ± 4.8%), and DL (4.60 ± 0.8%). The optimized SLNs (F2) was further evaluated by DSC, FTIR, SEM, in vitro release, and stability studies, which confirmed the successful encapsulation of ELX in SLNs. The efficacy of optimized SLNs (F2) in comparison to the pure ELX drug was assessed in acetic acid induced colitis rat models. It was observed that the delivery of ELX by SLNs alleviated the induced acetic acid colitis significantly. Thus, ELX loaded SLNs delivery to the colon has a significant potential to be developed for the treatment of ulcerative colitis.

scholarly journals FORMULATION AND CHARACTERIZATION OF PAPAIN LOADED SOLID LIPID NANOPARTICLES AGAINST HUMAN COLORECTAL ADENOCARCINOMA CELL LINE

2018 ◽  
Vol 11 (10) ◽  
pp. 393
Author(s):  
Suriyakala Perumal Chandran ◽  
Kannikaparameswari Nachimuthu
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Cell Viability ◽  
Cell Line ◽  
Solid Lipid Nanoparticles ◽  
Colorectal Adenocarcinoma ◽  
Lipid Nanoparticles ◽  
In Vitro Drug Release

Objective: Colorectal cancer is one of the most commonly diagnosed cancer and also most common gastrointestinal malignancy with high prevalence rate in the younger population. Usually, cancer cells are surrounded by a fibrin coat which is resistant to fibrinolytic degradation. This fibrin coat is act as self-protective against natural killing mechanism. The main objective was to prepare papain-loaded solid lipid nanoparticles (P-SLN) by melt dispersion-ultrasonication method and investigated the cytotoxic efficacy against colorectal adenocarcinoma (human colorectal adenocarcinoma [HCT 15]) cells.Methods: Optimized polymer ratio was characterized by differential scanning calorimetry, Fourier-transform infrared, X-ray diffraction, scanning electron microscopy, entrapment efficiency, particle size and zeta potential analysis, in vitro drug release, and in vitro cytotoxicity studies on HCT-15 colorectal adenocarcinoma cells.Results: The results showed that the particle size, morphological character and zeta potential value of optimized batch P-SLN were 265 nm, spherical and −26.5 Mv, respectively. The in vitro drug profile of P-SLN exhibited that it produced sustain drug release, and the cell viability of HCT-15 against P-SLN shown better efficacy than pure papain enzyme.Conclusion: P-SLNs were successfully prepared and investigated the in vitro drug release and in vitro cell viability against HCT-15 cell line.

scholarly journals FORMULATION AND EVALUATION OF DASATINIB LOADED SOLID LIPID NANOPARTICLES

2018 ◽  
Vol 10 (12) ◽  
pp. 14 ◽  
Author(s):  
M. Yasmin Begum ◽  
Prathyusha Reddy Gudipati
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Solid Lipid Nanoparticles ◽  
Entrapment Efficiency ◽  
Lipid Nanoparticles ◽  
Size Analysis ◽  
Compatibility Study ◽  
Solid Lipid ◽  
Poly Dispersity Index

Objective: The aim of present work was to formulate and evaluate Dasatinib (DST) loaded solid lipid nanoparticles (SLNs) as a potential anticancer drug delivery system by enhancing its solubility.Methods: SLNs consist of a solid lipid matrix where the drug was incorporated. Surfactants of GRAS grade were used to avoid aggregation and to stabilize the SLNs. DST-SLNs formulations of varying concentrations were prepared by high speed homogenization technique and evaluated for drug excipients compatibility study, poly-dispersity index, particle size analysis, surface morphology, zeta potential and drug release features.Results: It was observed that DST-SLNs with optimum quantities of poloxomer: lecithin ratio showed 88.06% drug release in 6h with good entrapment efficiency of 76.9±0.84 %. Particle size, Poly dispersity index, zeta potential and drug entrapment efficiency for the optimized formulation was found to be optimum. Stability studies revealed that the entrapment efficiency of the SLN dispersion stored in 4 °C was stable.Conclusion: Thus, it can be concluded that formulations of DST loaded SLNs are suitable carriers for improving the solubility and dissolution related problems. 

scholarly journals PREPARATION, PHYSICAL CHARACTERIZATION, AND PHARMACOKINETIC STUDY OF DOCETAXEL NANOCRYSTALS

2019 ◽  
pp. 238-244
Author(s):  
ARVIND GANNIMITTA ◽  
PRATHIMA SRINIVAS ◽  
VENKATESHWAR REDDY A ◽  
PEDIREDDI SOBHITA RANI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Water Solubility ◽  
Release Kinetics ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Sustained Drug Release ◽  
Egg Lecithin

Objective: The main objective of this study was to prepare and evaluate the nanocrystal formulation of docetaxel. Methods: Docetaxel nanocrystals were formulated to improve the water solubility. Docetaxel nanocrystals were prepared by nanoprecipitation method using Tween 80, egg lecithin, and povidone C-12 as stabilizers and poly(lactic-co-glycolic acid) (PLGA) as polymer in acceptable limits. A total of 16 formulations were prepared by changing stabilizer and polymer ratios. The prepared nanocrystals were characterized by particle size, zeta potential, crystalline structure, surface morphology, assay, saturation solubility, and in vitro drug release. Results: Based on particle size, polydispersity index, and zeta potential data, four formulations were optimized. The formulation containing Tween 80 as stabilizer has shown lowest particle size and better drug release than the formulations containing egg lecithin and povidone C-12 as stabilizers. The formulation containing Tween 80 and PLGA has shown still lower sized particles than the Tween 80 alone and exhibited prolonged sustained drug release. The release kinetics of formulations containing Tween 80 and PLGA followed zero-order release kinetics and formulations containing egg lecithin and povidone C-12 followed Higuchi diffusion (non-Fickian). Conclusion: From the study, we concluded that as the type and concentration of stabilizer changed the size and shape of the crystals were also changed and the formulations showed sustained drug release with non-Fickian diffusion.

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