Noscapine-loaded PLA Nanoparticles: Systematic Study of Effect of Formulation and Process Variables on Particle Size, Drug Loading and Entrapment Efficiency

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

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SCREENING OF BIODEGRADABLE POLYMER AND MOST EFFECTIVE VARIABLES IN PREPARATION OF ESSENTIAL OIL LOADED NANO PARTICLES FOR PULMONARY DELIVERY USING TAGUCHI DESIGN

INDIAN DRUGS ◽

10.53879/id.58.02.12664 ◽

2021 ◽

Vol 58 (02) ◽

pp. 68-75

Author(s):

Avani Khristi ◽

Lalit L. Jha ◽

Abhay Dharamsi ◽

Keyword(s):

Particle Size ◽

Essential Oil ◽

Biodegradable Polymers ◽

Drug Loading ◽

Pulmonary Inflammation ◽

Pulmonary Delivery ◽

Entrapment Efficiency ◽

Nano Particles ◽

Favorable Conditions ◽

Insoluble Polymers

The biodegradability of inhalable nanoparticles (NPs) is an important criterion in prevention of lung toxicity due to NPs which have been taken to cure the condition. Pulmonary inflammation may result due to non-biodegradation or insoluble polymers used to produce NPs. Biodegradable polymers are widely used for manufacturing safe drug-entrapped inhalable NPs for pulmonary delivery. Here in this study, for preparing ajwain essential oil loaded NPs for pulmonary delivery, biodegradable polymers chitosan, gelatin and alginic acid have been evaluated for suitability. Based on the results of trial batches prepared from each polymer, the responses particle size and entrapment efficiency were measured and compared. Out of the three polymers, chitosan was having very good entrapment efficiency, poly dispersive index, drug loading and zeta potential-favorable conditions for pulmonary delivery of essential oils. Further screening of most effective variables in manufacturing nano particles using chitosan, eight batches of nano particles have been prepared as per taguchi orthogonal 2 level array L8 experimental design (Design expert software, version 7.0) where two responses, particle size and entrapment efficiency, have been observed. Based on the results of eight batches, standard effects have been calculated and significant variables identified, for both particle size and entrapment efficiency, for further optimization under design of experiment.

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FORMULATION, OPTIMIZATION AND IN VITRO EVALUATION OF 5-FLUOROURACIL LOADED LIQUORICE CRUDE PROTEIN NANOPARTICLES FOR SUSTAINED DRUG DELIVERY USING BOX-BEHNKEN DESIGN

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2021v13i1.39932 ◽

2021 ◽

pp. 216-226

Author(s):

GEETHA V. S. ◽

MALARKODI VELRAJ

Keyword(s):

Drug Delivery ◽

Particle Size ◽

Drug Release ◽

Crude Protein ◽

Drug Loading ◽

Entrapment Efficiency ◽

Box Behnken Design ◽

Sustained Drug Delivery ◽

Drug Loading Efficiency

Objective: To formulate, optimize and evaluate 5-fluorouracil loaded liquorice crude protein nanoparticles for sustained drug delivery using Box-Behnken design. Methods: 5-fluorouracil (5-FU) loaded liquorice crude protein (LCP) nanoparticles were prepared by desolvation method using ethanol-water (1:2 ratio), Tween-80 (2%v/v) as stabilizing agent and gluteraldehyde (8% v/v) as cross linking agent. The optimization of prepared nanoparticles was carried out using Box-Behnken design with 3 factors 2 levels and 3 responses. The independent variables were A)5-FU concentration B)LCP concentration and C) sonication time while the responses were R1) Drug entrapment efficiency R2) Drug loading efficiency and R3) Particle size. The correlation between factors and responses were studied through response surface plots and mathematical equations. The nanoparticles were evaluated for FTIR, physicochemical properties like particle size and zeta potential by Photon correlation spectroscopy (PCS) and surface morphology by TEM. The entrapment efficiency, drug loading efficiency and in vitro drug release studies in PBS pH 7.4 (24 h) were carried out. The observed values were found to be in close agreement with the predicted value obtained from the optimization process. Results: 5-fluorouracil loaded LCP nanoparticles were prepared by desolvation method, the optimization was carried out by Box-Behnken design and the final formulation was evaluated for particle size (301.1 nm), zeta-potential (-25.8mV), PDI(0.226), with entrapment efficiency (64.07%), drug loading efficiency (28.54%), in vitro drug release (65.2% in 24 h) respectively. The formulated nanoparticles show Higuchi model drug release kinetics with sustained drug delivery for 24 h in pH7.4 buffer. Conclusion: The results were proved to be the most valuable for the sustained delivery of 5-Fluorouracil using liquorice crude protein as carrier. 5-FU–LCP nanoparticles were prepared using Tween-80 as stabilizing agent and gluteraldehyde as cross-linking agent to possess ideal sustained drug release characteristics.

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FORMULATION AND EVALUATION OF METFORMIN HYDROCHLORIDE LOADED FLOATING MICROSPHERES

International Journal of Pharmacy and Pharmaceutical Sciences ◽

10.22159/ijpps.2020v12i2.35099 ◽

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.

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FORMULATION AND EVALUATION OF ETHAMBUTOL POLYMERIC NANOPARTICLES

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2020v12i4.36845 ◽

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.

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PLGA nanoparticles simultaneously loaded with vincristine sulfate and verapamil hydrochloride: Systematic study of particle size and drug entrapment efficiency

International Journal of Pharmaceutics ◽

10.1016/j.ijpharm.2007.08.034 ◽

2008 ◽

Vol 350 (1-2) ◽

pp. 320-329 ◽

Cited By ~ 159

Author(s):

Xiangrong Song ◽

Yu Zhao ◽

Wenbin Wu ◽

Yueqi Bi ◽

Zheng Cai ◽

...

Keyword(s):

Particle Size ◽

Systematic Study ◽

Entrapment Efficiency ◽

Plga Nanoparticles ◽

Vincristine Sulfate ◽

Verapamil Hydrochloride ◽

Drug Entrapment Efficiency

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Preparation and Characterization of Solid Lipid Nanoparticles Loaded with Cisplatin

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i6.2033 ◽

2018 ◽

Vol 8 (6) ◽

pp. 125-131

Author(s):

Indrayani D. Raut ◽

Rajendra C. Doijad ◽

Shrinivas K. Mohite ◽

Arehalli S. Manjappa

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Solid Lipid Nanoparticles ◽

Drug Loading ◽

Acquired Resistance ◽

Spherical Shape ◽

Entrapment Efficiency ◽

Lipid Nanoparticles ◽

Platinum Drug ◽

Solid Lipid

Cisplatin (Cis diaminedichloro platinum) was the first platinum drug to be used as an anticancer drug, and it is widely used in the treatment of testicular, head, neck, ovarian and lung cancer. The use of Cisplatin is limited due to its intrinsic and acquired resistance and severe side effects such as chronic neurotoxicity and nephrotoxicity. The colloidal carriers such as emulsion, liposomes, polymeric nanoparticles have been extensively studied to overcome above limitations. The solid lipid nanoparticles (SLNs), amongst other colloidal carriers, were found to be an ideal carrier for lipophillic drug for better stability and release retardation. Cisplatin loaded solid lipid nanoparticles was prepared by microemulsion technique. Stearic acid was used as lipid. The other excipients were used as DPPG, Soya lecithin and Poloxamer P407 and acidic buffer PH4. Also used Probe sonication for 10 min at 79 Amplitude. Cisplatin SLNs Batch C13 showed particle size of 119.23±1.52 nm, Zeta potential of -37.33±2.47 mV, % Entrapment efficiency of 90.2 ± 2.1 %., % Drug loading capacity of 1.62 ± 1.34 %., The TEM study of optimized Cisplatin SLN illustrated the spherical shape of nanoparticles. Total release amount of Cisplatin was 82.62± 2.04 % after 48 hrs. The formulation performed kinetics study followed Peppas plot equation The SLNs of Cisplatin met all the requirements of a colloidal drug delivery system. They had particle size in nanosize; their size distribution was narrow and all the particles were in spherical shape and stable. Keywords: Cisplatin, Solid Lipid nanoparticles, zeta potential, Particle size, Transmission electron Microscopy.

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Gelatin Encapsulated Curcumin Nanoparticles Moderate Behavior of Human Primary Gingival Fibroblasts In Vitro

Journal of Nanomaterials ◽

10.1155/2020/2985721 ◽

2020 ◽

Vol 2020 ◽

pp. 1-11

Author(s):

Mai Thi-Hoang Nguyen ◽

Khanh Loan Ly ◽

Thoai Quoc Kieu ◽

Hiep Thi Nguyen ◽

Nam Cong-Nhat Huynh

Keyword(s):

Cell Proliferation ◽

Particle Size ◽

Drug Loading ◽

Entrapment Efficiency ◽

Gingival Fibroblasts ◽

Curcumin Nanoparticles ◽

Cell Proliferation And Migration ◽

And Migration ◽

Proliferation And Migration

Objective. Currently, there is no study evaluating the effect of nano-curcumin on human oral cells in vitro. In this study, we developed gelatin encapsulated curcumin nanoparticles (GelCur) and cultured the primary human gingival fibroblasts (hGFs) to verify the effect of GelCur on the cellular events related to oral wound healing capacities, such as cell migration and proliferation of gingival fibroblasts. Materials and Methods. GelCur was produced by the sonoprecipitation method. Particle size, zeta potential, SEM morphological observation, entrapment efficiency, and drug loading were used to characterize new GelCur. Primary hGFs were cultured from the attached gingival tissue of healthy third molar teeth. The effect of different concentrations of GelCur on hGFs was investigated by cell toxicity assay (MTT), cell proliferation assay, and cell migration assays by scratch test and transwell migration assay. Results. The average particle size of GelCur was around 356 nm with a moderate zeta potential of 26.5 mV. The mean PdI value of GelCur was 0.2, while the entrapment efficiency and drug loading of curcumin in this study were around 57% and 2.4%, respectively. IC30 of GelCur on hGFs was 3.96 mg/ml, while IC50 was 12,37 mg/ml. More than 70% of cells were viable after 24 hours incubated with 1, 2, and 3 mg/ml GelCur. At the concentration of 2 mg/ml GelCur virtually limited cell proliferation and migration. Conclusions. GelCur remained physically stable and did not alter cell proliferation and migration. The concentration of GelCur <3.96 mg/ml did not cause hGF cytotoxicity. Our study showed that within appropriate doses, GelCur can be used safely for hGFs.

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INFLUENCE OF SELECTED VARIABLES ON FABRICATION OF MUPIROCIN LOADED PLGA NANOCARRIERS

INDIAN DRUGS ◽

10.53879/id.54.05.10928 ◽

2017 ◽

Vol 54 (05) ◽

pp. 67-71

Author(s):

R. K Panik ◽

◽

M. R Singh ◽

D. Singh

Keyword(s):

Particle Size ◽

Surfactant Concentration ◽

Drug Loading ◽

Entrapment Efficiency ◽

Plga Nanoparticles ◽

Independent Variables ◽

Nanoprecipitation Method ◽

Dependent Variables ◽

Effective Delivery ◽

Polymer Ratio

Aim of the study was to develop PLGA nanoparticles (PLGA-NP) of mupirocin (MP) and to study the effect of independent variables in order to optimize the formulation for effective delivery. Drug loaded PLGA-NPs were successfully prepared by nanoprecipitation method and characterized by mean particle size, zeta potential, entrapment efficiency, drug loading, drug release, TEM, and DSC study. Independent variables like drug-polymer ratio, surfactant concentration, and stirring speed showed significant effect on the dependent variables like particle size, entrapment efficiency and drug loading. The ANOVA results showed that selected independent variables had a significant effect on the preparation of mupirocin loaded PLGA-NP.

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