FORMULATION AND EVALUATION OF LYCOPENE LOADED COLLOIDAL MICROPARTICLES GEL

Objective: The objective of the present investigation was to design and evaluate a gel containing lycopene loaded colloidal microparticles. Methods: The lycopene loaded colloidal microparticles were successfully prepared by Cloud point technique to form colloids using Tween 40 and Tween 60 surfactant solution and then incorporated into microparticles by solvent evaporation method using polymer like HPMC and ethyl cellulose. These colloidal microparticles were evaluated for particle size (PS), drug loading (DL), entrapment efficiency (EE), Scanning Electron Microscopy (SEM). Further, these colloidal microparticles were incorporated into a topical formulation i.e., gel. This topical formulation was then evaluated for macroscopic examination, viscosity, drug content, spreadability, antioxidant activity, in vitro permeation and release kinetics. Results: Colloidal microparticles were successfully prepared and the particle size, drug loading and entrapment efficiency were found to be 249.45±14.2 μm, 49.8±0.96 % and 93.4±0.26 % respectively. FTIR study depicted no chemical interaction between pure drug lycopene and other excipients. The topical formulation showed sustained release and followed Korsmeyer-Peppas release kinetics model. Conclusion: The sustained release topical formulation of lycopene was successfully prepared using Tween 40 and Tween 60 surfactant solution and combination of HPMC and ethyl cellulose and evaluated for several parameters.

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FORMULATION AND EVALUATION OF MUCOADHESIVE MICROSPHERES OF AN ANTI-MIGRAINE DRUG

Journal of Drug Delivery and Therapeutics ◽

10.22270/jddt.v8i5.1943 ◽

2018 ◽

Vol 8 (5) ◽

pp. 465-474

Author(s):

S PADMA PRIYA ◽

AN Rajalakshmi ◽

P Ilaveni

Keyword(s):

Drug Release ◽

Sustained Release ◽

Sodium Alginate ◽

Release Kinetics ◽

Drug Loading ◽

Research Work ◽

Entrapment Efficiency ◽

Polyvinyl Pyrrolidone ◽

Anti Migraine Drug

Objective: The objective of this research work is to develop and evaluate mucoadhesive microspheres of an anti-migraine drug for sustained release. Materials and Methods: Mucoadhesive microspheres were prepared by emulsification method using Sodium alginate (SA), polyvinyl pyrrolidone (PVP) and Chitosan in the various drug-polymer ratios of 1:1, 1:2 and 1:3. Nine formulations were formulated and evaluated for possible drug polymer interactions, percentage yield, micromeritic properties, particle size, drug content, drug entrapment efficiency, drug loading, swelling index, In-vitro wash off test, in vitro drug release, surface morphology and release kinetics. Results: The results showed that no significant drug polymer interaction in FTIR studies. Among all the formulations SF3 containing sodium alginate showed 77.18% drug release in 6hrs. Conclusion: Amongst the developed mucoadhesive microspheres, SF3 formulation containing sodium alginate exhibited slow and sustained release in a controlled manner and it is a promising formulation for sustained release of Sumatriptan succinate. Keywords: Mucoadhesive microspheres, Sodium alginate, polyvinyl pyrrolidone, Chitosan, sustained release.

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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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Development of Oral Sustained Release Rifampicin Loaded Chitosan Nanoparticles by Design of Experiment

Journal of Drug Delivery ◽

10.1155/2013/370938 ◽

2013 ◽

Vol 2013 ◽

pp. 1-10 ◽

Cited By ~ 30

Author(s):

Bhavin K. Patel ◽

Rajesh H. Parikh ◽

Pooja S. Aboti

Keyword(s):

Particle Size ◽

Drug Release ◽

Sustained Release ◽

Design Of Experiment ◽

Drug Loading ◽

Chitosan Nanoparticles ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Release Kinetic

Objective. The main objective of the present investigation was to develop and optimize oral sustained release Chitosan nanoparticles (CNs) of rifampicin by design of experiment (DOE). Methodology. CNs were prepared by modified emulsion ionic gelation technique. Here, inclusion of hydrophobic drug moiety in the hydrophilic matrix of polymer is applied for rifampicin delivery using CN. The 23 full-factorial design was employed by selecting the independent variables such as Chitosan concentration (X1), concentration of tripolyphosphate (X2), and homogenization speed (X3) in order to achieve desired particle size with maximum percent entrapment efficiency and drug loading. The design was validated by checkpoint analysis, and formulation was optimized using the desirability function. Results. Particle size, drug entrapment efficiency, and drug loading for the optimized batch were found to be 221.9 nm, 44.17 ± 1.98% W/W, and 42.96 ± 2.91% W/W, respectively. In vitro release data of optimized formulation showed an initial burst followed by slow sustained drug release. Kinetic drug release from CNs was best fitted to Higuchi model. Conclusion. Design of Experiment is an important tool for obtaining desired characteristics of rifampicin loaded CNs. In vitro study suggests that oral sustained release CNs might be an effective drug delivery system for tuberculosis.

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FORMULATION AND EVALUATION OF ALLOPURINOL LOADED CHITOSAN NANOPARTICLES

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i3.31932 ◽

2019 ◽

pp. 49-52 ◽

Cited By ~ 3

Author(s):

Gurpreet Kandav ◽

D.c. Bhatt ◽

Deepak Kumar Jindal

Keyword(s):

Particle Size ◽

Drug Release ◽

Sustained Release ◽

Release Kinetics ◽

Chitosan Nanoparticles ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Polydispersity Index ◽

Sustained Release Formulation

Objective: The objective of the present investigation was to fabricate and characterize allopurinol loaded chitosan nanoparticles (A-CNPs) for sustained release of drug. Methods: The allopurinol loaded chitosan nanoparticles were successfully prepared by employing the ionotropic gelation method. Further, particle size (PS), polydispersity index (PDI), zeta potential (ZP), Differential Scanning Calorimetry (DSC), entrapment efficiency (EE), Transmission Electron Microscopy (TEM), in vitro drug release, X-Ray Diffraction (XRD) and Fourier transform infrared (FTIR) were used for evaluating formulated A-CNPs Results: A-CNPs was successfully prepared and the particle size, polydispersity index, ZP and entrapment efficiency were found to be 375.3±10.1 nm, 0.362±0.01 and 32.5±2.7 mV and 52.56±0.10% respectively. In vitro release profile of A-CNPs showed sustained release and Higuchi model was found to be best fit for drug release kinetics. FTIR study depicted no chemical interaction between pure drug allopurinol (AL) and other excipients. Conclusion: The sustained release formulation of allopurinol was successfully prepared using HMW chitosan and evaluated for different parameters.

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FORMULATION, OPTIMIZATION, AND CHARACTERIZATION OF BIOCOMPATIBLE INHALABLE D-CYCLOSERINE-LOADED ALGINATE-CHITOSAN NANOPARTICLES FOR PULMONARY DRUG DELIVERY

Asian Journal of Pharmaceutical and Clinical Research ◽

10.22159/ajpcr.2016.v9s2.11814 ◽

2016 ◽

pp. 82 ◽

Cited By ~ 4

Author(s):

Jessy Shaji ◽

Mahmood Shaikh

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Sustained Release ◽

Drug Loading ◽

Chitosan Nanoparticles ◽

Entrapment Efficiency ◽

Drug Bioavailability ◽

Scanning Calorimetry ◽

Ionotropic Gelation ◽

Mdr Tb

ABSTRACT Objective: To prepare Nanoparticulate dosage form having improved drug bioavailability and reduced dosing frequency of antitubercular drugs which will helps in improving patient compliance in the treatment of multi-drug resistant tuberculosis (MDR-TB). Methods: Ionotropic gelation method was used to prepare D-cycloserine (D-CS)-loaded alginate-chitosan nanoparticles, and the particles are characterized by their particle size and morphology using particle size analyzer and scanning electron microscopy (SEM). X-ray diffraction (XRD), differential scanning calorimetry (DSC), and Fourier-transformed infrared (FTIR) studies were used to determine drug-polymer interactions and drug entrapment. Entrapment efficiency, drug loading (DL), particle size, and zeta potential of nanoparticles were also studied. The 2 factorial designs of experiments by Design-Expert ® V9 were used to optimize the particle size and entrapment efficiency of nanoparticles. Results: The optimized batch had shown the entrapment efficiency of 98.10±0.24% and DL of 69.32±0.44% with particle size and zeta potential as 344±5 nm and −42±11.40 mV, respectively. DSC, FTIR, and XRD studies confirmed the drug entrapment within nanoparticle matrix. SEM results showed spherical-shaped particles. Sustained release of drug from the nanoparticles was observed for 24 hrs period. Respirable fraction up to 52.37±0.7% demonstrates the formulation suitability for deep lung delivery. Lung inflammatory study showed a less inflammatory response. Conclusion: Ionotropic gelation method can be used to prepare biocompatible particles with a high entrapment efficiency, DL, optimum particle size, and controlled release characteristics, which can serve as a convenient delivery system for D-CS and could be a potential alternative to the existing conventional therapy in MDR-TB. Keywords: Nanoparticles, Alginate, Chitosan, Inhalation, Sustained release, Tuberculosis. 3

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Formulation and Evaluation of Mefloquine Hydrochloride Nanoparticles

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2014.7.1.10 ◽

2014 ◽

Vol 7 (1) ◽

pp. 2377-2386

Author(s):

Dilip Kumar Gupta ◽

B K Razdan ◽

Meenakshi Bajpai

Keyword(s):

Particle Size ◽

Sustained Release ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Taste Masking ◽

Diffusion Method ◽

Drug Entrapment Efficiency ◽

Resistant Strains ◽

Vitro Release

The present study deals with the formulation and evaluation of mefloquine hydrochloride nanoparticles. Mefloquine is a blood schizonticidal quinoline compound, which is indicated for the treatment of mild-to-moderate acute malarial infections caused by mefloquine-susceptible multi-resistant strains of P. falciparum and P. vivax. The purpose of the present work is to minimize the dosing frequency, taste masking toxicity and to improve the therapeutic efficacy by formulating mefloquine HCl nanoparticles. Mefloquine nanoparticles were formulated by emulsion diffusion method using polymer poly(ε-caprolactone) with six different formulations. Nanoparticles were characterized by determining its particle size, polydispersity index, drug entrapment efficiency, drug content, particle morphological character and drug release. The particle size ranged between 100 nm to 240 nm. Drug entrapment efficacy was >95%. The in-vitro release of nanoparticles were carried out which exhibited a sustained release of mefloquine HCl from nanoparticles up to 24 hrs. The results showed that nanoparticles can be a promising drug delivery system for sustained release of mefloquine HCl.

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

International Journal of Pharmaceutical Sciences and Nanotechnology ◽

10.37285/ijpsn.2019.12.2.5 ◽

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

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Development of In Situ Self-Assembly Nanoparticles to Encapsulate Lopinavir and Ritonavir for Long-Acting Subcutaneous Injection

Pharmaceutics ◽

10.3390/pharmaceutics13060904 ◽

2021 ◽

Vol 13 (6) ◽

pp. 904

Author(s):

Irin Tanaudommongkon ◽

Asama Tanaudommongkon ◽

Xiaowei Dong

Keyword(s):

Sustained Release ◽

Trough Concentration ◽

Self Assembly ◽

Subcutaneous Injection ◽

Drug Loading ◽

Entrapment Efficiency ◽

Long Acting

Most antiretroviral medications for human immunodeficiency virus treatment and prevention require high levels of patient adherence, such that medications need to be administered daily without missing doses. Here, a long-acting subcutaneous injection of lopinavir (LPV) in combination with ritonavir (RTV) using in situ self-assembly nanoparticles (ISNPs) was developed to potentially overcome adherence barriers. The ISNP approach can improve the pharmacokinetic profiles of the drugs. The ISNPs were characterized in terms of particle size, drug entrapment efficiency, drug loading, in vitro release study, and in vivo pharmacokinetic study. LPV/RTV ISNPs were 167.8 nm in size, with a polydispersity index of less than 0.35. The entrapment efficiency was over 98% for both LPV and RTV, with drug loadings of 25% LPV and 6.3% RTV. A slow release rate of LPV was observed at about 20% on day 5, followed by a sustained release beyond 14 days. RTV released faster than LPV in the first 5 days and slower than LPV thereafter. LPV trough concentration remained above 160 ng/mL and RTV trough concentration was above 50 ng/mL after 6 days with one subcutaneous injection. Overall, the ISNP-based LPV/RTV injection showed sustained release profiles in both in vitro and in vivo studies.

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FORMULATION AND CHARACTERIZATION OF TIMOLOL MALEATE-LOADED NANOPARTICLES GEL BY IONIC GELATION METHOD USING CHITOSAN AND SODIUM ALGINATE

International Journal of Applied Pharmaceutics ◽

10.22159/ijap.2019v11i6.34983 ◽

2019 ◽

pp. 48-54 ◽

Cited By ~ 1

Author(s):

RISA AHDYANI ◽

LARAS NOVITASARI ◽

RONNY MARTIEN

Keyword(s):

Particle Size ◽

Zeta Potential ◽

Sodium Alginate ◽

Release Kinetics ◽

In Vitro Release ◽

Entrapment Efficiency ◽

Polydispersity Index ◽

Ionic Gelation ◽

Timolol Maleate ◽

Optimum Formula

Objective: The objectives of this study were to formulate and characterize nanoparticles gel of timolol maleate (TM) by ionic gelation method using chitosan (CS) and sodium alginate (SA). Methods: Optimization was carried out by factorial design using Design Expert®10.0.1 software to obtain the concentration of CS, SA, and calcium chloride (CaCl2) to produce the optimum formula of TM nanoparticles. The optimum formula was characterized for particle size, polydispersity index, entrapment efficiency, Zeta potential, and molecular structure. Hydroxy Propyl Methyl Cellulose (HPMC) K15 was incorporated into optimum formula to form nanoparticles gel of TM and carried out in vivo release study using the Franz Diffusion Cell. Results: TM nanoparticles was successfully prepared with concentration of CS, SA, and CaCl2 of 0.01 % (w/v), 0.1 % (w/v), and 0.25 % (w/v), respectively. The particle size, polydispersity index, entrapment efficiency, and Zeta potential were found to be 200.47±4.20 nm, 0.27±0.0154, 35.23±4.55 %, and-5.68±1.80 mV, respectively. The result of FTIR spectra indicated TM-loaded in the nanoparticles system. In vitro release profile of TM-loaded nanoparticles gel showed controlled release and the Korsmeyer-Peppas model was found to be the best fit for drug release kinetics. Conclusion: TM-loaded CS/SA nanoparticles gel was successfully prepared and could be considered as a promising candidate for controlled TM delivery of infantile hemangioma treatment.

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