Formulation and Evaluation of Lovastatin Loaded Nanosponges for the treatment of Hyperlipidemia

2021 ◽  
pp. 5653-5660
Author(s):  
Ranjitha R ◽  
Elango K ◽  
Devi Damayanthi R ◽  
Sahul Hameed Niyaz U
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Entrapment Efficiency ◽  
Flow Property ◽  
Water Soluble ◽  
Fickian Diffusion ◽  
Average Particle ◽  
Stability Studies ◽  
Formulation Parameters

The present investigations was aimed to improve the solubility, to release the drug in a controlled manner for extended period of time, reduce dose dependent side effects and improve the bioavailability of a poorly water soluble BCS class II drug of Lovastatin by formulating it as Nanosponges drug delivery system. Lovastatin Nanosponges were formulated by emulsion solvent evaporation method using Eudragit RS 100 and Ethyl Cellulose as a polymers, PVA as a stabilizer and finally enclosed in hard gelatin Capsules. The prepared Nanosponges were evaluated for FTIR, particle size, polydispersity index (PDI), zeta potential, morphological characteristics by scanning electron microscopy (SEM), production yield, entrapment efficiency, solubility studies, in vitro drug release studies, release kinetics study, stability studies, Flow property and porosity. The optimized formulation filled in capsules and Post formulation parameters of capsule were determined. FTIR studies showed no interaction between drug and excipients. Percentage yield of all the formulation (F1-F10) was found to be in the range of 85.83 to 99.85%. The entrapment efficiency of all the formulations was found to be in the range of 61.68 to 91.18%, among all the formulations F3 (90.04%) and F8 (91.18%) shows high entrapment efficiency. The solubility of all formulation improved (from insoluble to slightly soluble) compared to pure drug of Lovastatin. Among all the formulations F3 (98.15%) and F8 (97.57%) shown complete drug release at the end of 12th hrs. The average particle size of optimized formulation F3 and F8 was found to be 727.0 nm and 769.5 nm respectively. SEM images of optimized formulation showed that the Nanosponges were spherical with numerous pores on their surface, uniform and spongy in nature. The release kinetics of the optimized formulation was best fitted into Higuchi model and showed zero order drug release with Non Fickian diffusion. Stability studies indicated that the formulation is stable as per ICH guidelines. The flow property measurements for optimized formulation observed good were its filled in capsules. Post formulation parameters of capsule were comply with official specifications. They concluded that the both polymers used were efficient carriers for Lovastatin Nanosponges.

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.

FORMULATION, CHARACTERIZATION AND IN VITRO EVALUTION OF GABAPENTIN FLOATING MICROSPHERES

INDIAN DRUGS ◽  
2017 ◽  
Vol 54 (01) ◽  
pp. 20-27
Author(s):  
H. B Samal ◽  
I. J. Das ◽  
P. N. Murthy ◽  
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Polymer Concentration ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Linear Regression Method ◽  
Average Particle ◽  
Drug Entrapment Efficiency

The present study involves the design and characterization of floating microspheres with gabapentin as model drug for prolongation of gastric residence time. Gabapentin floating microspheres were prepared by o/w/o emulsification solvent diffusion technique using ethyl cellulose as the rate controlling polymer at various concentrations. The shape and surface morphology of microspheres were characterized by optical and scanning electron microscopy. Absence of drug-polymer interaction was confirmed by FTIR analysis. In vitro drug release studies were performed and drug release kinetics was evaluated using the linear regression method. Effects of polymer concentration, solvent composition, particle size, drug entrapment efficiency and drug release were also studied. The synthesized microspheres exhibited prolonged drug release (> 12 h) and remained buoyant for > 24 h. The drug entrapment efficiency was in the range 46-70 %. At higher polymer concentration, the average particle size was increased and the drug release rate decreased. In vitro studies revealed diffusion-controlled drug release from the microspheres. Among all the formulations (F1-F5), F4 is the optimized formulation.

scholarly journals FORMULATION AND EVALUATION OF LORNOXICAM MICROSPONGES USING EUDRAGIT RS 100 AND EUDRAGIT RSPO

2018 ◽  
Vol 11 (10) ◽  
pp. 217
Author(s):  
Bannaravuri Thireesha ◽  
Ayya Rajendra Prasad ◽  
Haroled Peter P L
Keyword(s):  
Rheumatoid Arthritis ◽  
Particle Size ◽  
Drug Release ◽  
Entrapment Efficiency ◽  
Fickian Diffusion ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Eudragit Rs ◽  
Percentage Yield

Objective: The objective of the present study was preparation and evaluation of lornoxicam microsponges to prolong their drug release up to 12 h for effective osteoarthritis, rheumatoid arthritis, and acute lumbar-sciatica therapy.Methods: Lornoxicam microsponges were prepared by the quasi-emulsion solvent diffusion technique using different concentrations of polymers such as Eudragit RS 100 and Eudragit RSPO in ethanol and dichloromethane organic solvent mixture. Microsponges were evaluated for their particle size, percentage yield, entrapment efficiency, scanning electron microscopy (SEM), and in vitro drug release studies.Results: The percentage yield, entrapment efficiency, average particle size, and in vitro drug release for optimized formulation F12 were found to be 70.23% w/w, 81.34% w/w, 172.72 μm, and 96.64% up to 8 h, respectively. From SEM, it was observed that microsponges were found to be spherical in shape with rough surface texture. The formulation F12 shows zero-order release kinetics with an r2 value of 0.961 and the value of Korsmeyer–Peppas model was found to be 0.792; it follows super case II non-Fickian diffusion. The in vitro drug release studies showed that formulations comprised varying concentrations of Eudragit RSPO in higher proportion exhibited much-retarded drug release as compared to formulations comprised a higher proportion of varying concentrations of Eudragit RS 100.Conclusion: Among all the formulations F12 shows better results, which are released more than 80% of the drug release within 8 h; hence, it is optimized. These developed microsponges are releasing the drug for a longer period, which will be effective for osteoarthritis, rheumatoid arthritis, and acute lumbar sciatica therapy.

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

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.

scholarly journals FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE LOADED FLOATING MICROSPHERES

2019 ◽  
pp. 74-82
Author(s):  
SHIKHA KESHARVANI ◽  
PANKAJ KUMAR JAISWAL ◽  
ALOK MUKERJEE ◽  
AMIT KUMAR SINGH
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Surface Morphology ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Metformin Hydrochloride ◽  
Compatibility Study ◽  
Specific Drug ◽  
Site Specific

Objective: The main objective of this study was to develop and evaluate the eudragit and HPMC coated metformin hydrochloride floating microspheres, in which HPMC helps in floating and eudragit as a coating material for a site-specific drug release in a controlled manner and the active moiety metformin used as anti-hyperglycemic agent. Methods: The floating microsphere was prepared by the solvent evaporation method incorporating metformin as a model drug. The prepared floating microsphere were characterized for particle size, %yield, drug loading and entrapment efficiency, compatibility study, %buoyancy, surface morphology and In vitro drug release and release kinetics. Results: The result metformin loaded floating microsphere was successfully prepared and the particle size range from 397±23.22 to 595±15.82 µm, the entrapment efficiency range from 83.49±1.33 to 60.02±1.65% and drug loading capacity range from 14.3±0.54 to 13.31±0.47% and %buoyancy range from 85.67±0.58 to 80.67±1.15%. The FT-IR and X-RD analysis confirmed that no any interaction between drug and excipient, and surface morphology confirmed those particles are sphere. The floating microsphere show maximum 96% drug release in pH 0.1N HCL and follow the Korsmeyer peppas model of the super case-2 transport mechanism. Conclusion: These results suggest that metformin loaded floating microspheres could be retain in stomach for long time and give site specific drug release in controlled manner.

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.

scholarly journals Fabrication and in vitro characterization of polymeric nanoparticles for Parkinson's therapy: a novel approach

2014 ◽  
Vol 50 (4) ◽  
pp. 869-876 ◽  
Author(s):  
Neha Gulati ◽  
Upendra Nagaich ◽  
Shubhini Saraf
Keyword(s):  
Drug Release ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Mode Of Delivery ◽  
Chitosan Nanoparticles ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Fickian Diffusion ◽  
Novel Approach

The objective of the research was to formulate and evaluate selegiline hydrochloride loaded chitosan nanoparticles for the Parkinson's therapy in order to improve its therapeutic effect and reducing dosing frequency. Taguchi method of design of experiments (L9 orthogonal array) was used to get optimized formulation. The selegiline hydrochloride loaded chitosan nanoparticles (SHPs) were prepared by ionic gelation of chitosan with tripolyphosphate anions (TPP) and tween 80 as surfactant. The SHPs had a mean size of (303.39 ± 2.01) nm, a zeta potential of +32.50mV, and entrapment efficiency of SHPs was 86.200 ± 1.38%. The in vitro drug release of SHPs was evaluated in phosphate buffer saline (pH 5.5) using goat nasal mucosa and found to be 82.529% ± 1.308 up to 28 h. Release kinetics studies showed that the release of drug from nanoparticles was anomalous (non-fickian) diffusion indicating the drug release is controlled by more than one process i.e. superposition of both phenomenon, the diffusion controlled as well as swelling controlled release. SHPs showed good stability results as found during stability studies at different temperatures as mentioned in ICH guidelines. The results revealed that selegiline hydrochloride loaded chitosan nanoparticles are most suitable mode of delivery of drug for promising therapeutic action.

scholarly journals FORMULATION AND EVALUATION OF ETHAMBUTOL POLYMERIC NANOPARTICLES

2020 ◽  
pp. 207-217
Author(s):  
MONOWAR HUSSAIN ◽  
ANUPAM SARMA ◽  
SHEIKH SOFIUR RAHMAN ◽  
ABDUL MATIN SIDDIQUE ◽  
TANUKU PAVANI EESWARI
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymeric Nanoparticles ◽  
Release Kinetics ◽  
Drug Loading ◽  
Entrapment Efficiency ◽  
Compatibility Study ◽  
Bacterial Disease ◽  
Dose Frequency

Objective: Tuberculosis (TB) is an infectious bacterial disease caused by Mycobacterium tuberculosis which most commonly affects the lungs. TB has the highest mortality rate than any other infectious disease occurs worldwide. The main objective of the present investigation was to develop polymeric nanoparticles based drug delivery system to sustain the ethambutol (ETB) release by reducing the dose frequency. Methods: The Preformulation studies of drug ETB were done by physical characterization, melting point determination, and UV spectrophotometric analysis. The ETB loaded nanoparticles were prepared by double-emulsion (W/O/W) solvent evaporation/diffusion technique. The prepared polymeric nanoparticles were evaluated for particle size, polydispersity index, zeta potential, drug entrapment efficiency, drug loading, drug-polymer compatibility study, surface morphology, in vitro drug release, and release kinetics. Results: Based on the result obtained from the prepared formulations, F11 showed the best result and was selected as the optimized formulation. Optimized batch (F11) showed better entrapment efficiency (73.3%), good drug loading capacity (13.21%), optimum particle size (136.1 nm), and zeta potential (25.2 mV) with % cumulative drug release of 79.08% at the end of 24 h. Conclusion: These results attributed that developed polymeric nanoparticles could be effective in sustaining the ETB release over 24 h. Moreover, the developed nanoparticles could be an alternate method for ETB delivery with a prolonged drug release profile and a better therapeutic effect can be achieved for the treatment of tuberculosis.

scholarly journals FLUCONAZOLE NANOGEL: FABRICATION AND IN VITRO EVALUATION FOR TOPICAL APPLICATION

2021 ◽  
pp. 272-277
Author(s):  
DIVYA ◽  
INDERBIR SINGH ◽  
UPENDRA NAGAICH
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Seborrheic Dermatitis ◽  
In Vitro Release ◽  
Entrapment Efficiency ◽  
Tween 80 ◽  
Flow Index ◽  
In Vitro Evaluation

Objective: The aim of this study is to develop and in vitro evaluation of prepared fluconazole nanogel for seborrheic dermatitis Methods: Fluconazole nanogel was formulated to act against seborrheic dermatitis. The fluconazole nanoparticles were prepared by a simplified evaporation method and evaluated for particle size, entrapment efficiency, and percent in vitro drug release. The nanogel was also characterized based on parameters like particle size, percent entrapment efficiency, shape surface morphology, rheological properties, in vitro release R² = 0.9046, and release kinetics. Results: The nanoparticle with a combination of Eudragit RS and Tween 80 showed the best result with particle size in the range of 119.0 nm to 149.5 nm, with a cumulative percent drug release of 95 % up to 18 h. The formulated nanogel with optimum concentration of HPMC authenticate with particle size 149.50±0.5 with maximum drug release (92.13±0.32) %. Conclusion: Different percentages of polymers (ethyl-cellulose, eudragit, and tween 80) are used as variable components in the formulation of nanogel. The optimized batch showed good physical properties (flow index, spreadability, and viscosity) along with rapid drug release. Therefore, it can be concluded that nanogel containing fluconazole has potential application in topical delivery.

scholarly journals INVESTIGATION ON DISSOLUTION PATTERN AND MATHEMATICAL MODELING OF DRUG RELEASE OF QUERCETIN BY COMPLEXATION WITH CYCLODEXTRIN NANOSPONGES

2019 ◽  
pp. 260-264
Author(s):  
SOBITHARANI P ◽  
ANANDAM S ◽  
MOHAN VARMA M ◽  
VIJAYA RATNA J ◽  
SHAILAJA P
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Average Particle Size ◽  
Particle Size Analysis ◽  
Water Soluble ◽  
Size Analysis ◽  
Average Particle ◽  
Scattering Method ◽  
Release Pattern ◽  
Cyclodextrin Nanosponges

Objective: The main objective of this study was to investigate the release pattern of a poorly water-soluble drug quercetin (QU) by fabricating its cyclodextrin nanosponges. Methods: Characterization of the original QU powder and QU-loaded nanosponges was carried out by the Fourier-transformed infrared (FTIR) spectroscopy, transmission electron microscopy (TEM), and dissolution tester. The drug release pattern was subjected to various kinetic models. Results: FTIR studies confirmed the formation of inclusion complex of drug. The particle size analysis revealed that the average particle size measured by laser light scattering method is around 400–420 nm with low polydispersity index. The particle size distribution is unimodal and having a narrow range. A sufficiently high zeta potential indicates that the complexes would be stable and the tendency to agglomerate would be miniscule. TEM image revealed the porous nature of nanosponges. The dissolution of the QU nanosponges was significantly higher compared with the pure drug. Conclusion: From the kinetic study, it is apparent that the regression coefficient value closer to unity in case of Korsmeyer-Peppas model indicates that the drug release exponentially to the elapsed time. n value obtained from the Korsmeyer-Peppas plots, i.e., 0.9911 indicating non-Fickian (anomalous) transport ; thus, it projected that delivered its active ingredient by coupled diffusion and erosion.

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