FORMULATION AND EVALUATION OF CAPTOPRIL BIOADHESIVE MICROSPHERES

INDIAN DRUGS ◽  
2021 ◽  
Vol 58 (09) ◽  
pp. 70-72
Author(s):  
Sridevi Gowripattapu ◽  
◽  
Anusha Nallamilli ◽  
Ashokbabu K. S
Keyword(s):  
Particle Size ◽  
Polymer Concentration ◽  
Oral Route ◽  
Aqueous System ◽  
Residual Solvents ◽  
Ionotropic Gelation ◽  
Effi Ciency ◽  
Microsphere Method ◽  
The Mean

In the present work, captopril microspheres using HPMCK100M, HPMCK15M and Carbopol 934 as copolymers were formulated by ionic cross linking technique (ionotropic gelation method) to deliver captopril via oral route. The technique was successfully employed to fabricate captopril microspheres and provides characteristic advantage over conventional microsphere method, which involves an “all-aqueous” system and thus avoids residual solvents in microspheres. Other methods utilize larger volume of organic solvents are costly and hazardous. Micromeritic studies revealed that the mean particle size was in the range of 512-903 μm. Increase in the polymer concentration led to increase in % yield, % drug entrapment effi ciency, particle size, % swelling and % mucoadhesion. The in vitro mucoadhesive study demonstrated that captopril microspheres using sodium alginate along with HPMCK100M as copolymer adhered to the mucus to a greater extent than the microspheres of captopril using albumin along with HPMCK15M and Carbopol 934 as copolymers.

Formulation and Evaluation of Benidipine Nanosuspension

2021 ◽  
pp. 4111-4116
Author(s):  
Sejal Patel ◽  
Anita P. Patel
Keyword(s):  
Particle Size ◽  
Water Solubility ◽  
Polymer Concentration ◽  
Oral Route ◽  
Water Soluble ◽  
In Vitro Dissolution ◽  
Scanning Calorimetry ◽  
23 Factorial Design ◽  
Selection Of

In the interest of administration of dosage form oral route is most desirable and preferred method. After oral administration to get maximum therapeutic effect, major challenge is their water solubility. Water insoluble drug indicate insufficient bioavailability as well dissolution resulting in fluctuating plasma level. Benidipine (BND) is poorly water soluble antihypertensive drug has lower bioavailability. To improve bioavailability of Benidipine HCL, BND nanosuspension was formulated using media milling technique. HPMC E5 was used to stabilize nanosuspension. The effect of different important process parameters e.g. selection of polymer concentration X1(1.25 mg), stirring time X2 (800 rpm), selection of zirconium beads size X3 (0.4mm) were investigated by 23 factorial design to accomplish desired particle size and saturation solubility. The optimized batch had 408 nm particle size Y1, and showed in-vitro dissolution Y2 95±0.26 % in 30 mins and Zeta potential was -19.6. Differential scanning calorimetry (DSC) and FT-IR analysis was done to confirm there was no interaction between drug and polymer.

scholarly journals Formulation and invitro evaluation of oral extended release microspheres of aceclofenac using various natural polymers

2019 ◽  
Vol 1 (2) ◽  
pp. 58-66
Author(s):  
Syed abid ali ◽  
Syed mujtaba pasha ◽  
Omair sohail ahmed ◽  
Omer wasiq ◽  
Mohammed mukaram ◽  
...  
Keyword(s):  
Drug Release ◽  
Sodium Alginate ◽  
Oral Route ◽  
Aqueous System ◽  
Fickian Diffusion ◽  
Release Mechanism ◽  
Natural Polymers ◽  
Drug Release Mechanism ◽  
Microsphere Method

In the present work, bioadhesive microspheres of Aceclofenac using Sodium alginate along with Carbopol 934, Carbopol 971, HPMC K4M as copolymers were formulated to deliver Aceclofenac via oral route. The results of this investigation indicate that ionic cross-linking technique Ionotropic gelation method can be successfully employed to fabricate Aceclofenac microspheres. The technique provides characteristic advantage over conventional microsphere method, which involves an “all-aqueous” system, avoids residual solvents in microspheres. FT-IR spectra of the physical mixture revealed that the drug is compatible with the polymers and copolymers used. Micromeritic studies revealed that the mean particle size of the prepared microspheres was in the size range of 512-903µm and are suitable for bioadhesive microspheres for oral administration. The in-vitro mucoadhesive study demonstrated that microspheres of Aceclofenac using sodium alginate along with Carbopol934 as copolymer adhered to the mucus to a greater extent than the microspheres of Aceclofenac using sodium alginate along with Carbopol 971 and HPMC K4M as copolymers. The invitro drug release decreased with increase in the polymer and copolymer concentration. Analysis of drug release mechanism showed that the drug release from the formulations followed non-Fickian diffusion and the best fit model was found to be Korsmeyer-Peppas. Based on the results of evaluation tests formulation coded T4 was concluded as best formulation.

scholarly journals Sodium Alginate Nanoparticles of Isoniazid: Preparation and Evaluation

2019 ◽  
Vol 11 (06) ◽  
Author(s):  
Sumit Kumar ◽  
Dinesh Chandra Bhatt
Keyword(s):  
Particle Size ◽  
Sodium Alginate ◽  
Encapsulation Efficiency ◽  
Drug Loading ◽  
Average Particle Size ◽  
Average Particle ◽  
In Vitro Drug Release ◽  
Ionotropic Gelation ◽  
Preparation And Evaluation

Fabrication and evaluation of the Isoniazid loaded sodium alginate nanoparticles (NPs) was main objective of current investigation. These NPs were engineered using ionotropic gelation technique. The NPs fabricated, were evaluated for average particle size, encapsulation efficiency, drug loading, and FTIR spectroscopy along with in vitro drug release. The particle size, drug loading and encapsulation efficiency of fabricated nanoparticles were ranging from 230.7 to 532.1 nm, 5.88% to 11.37% and 30.29% to 59.70% respectively. Amongst all batches studied formulation F-8 showed the best sustained release of drug at the end of 24 hours.

scholarly journals Preparation and preclinical evaluation of aceclofenac loaded pectinate mucoadhesive microspheres

2012 ◽  
Vol 2 (1) ◽  
pp. 8 ◽  
Author(s):  
Santanu Chakraborty ◽  
Priyanka Nayak ◽  
Bala Murali Krishna ◽  
Madhusmruti Khandai ◽  
Ashoke Kumar Ghosh
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Polymer Concentration ◽  
Research Work ◽  
In Vivo Studies ◽  
Systemic Absorption ◽  
Cross Linking ◽  
Significant Difference

The aim of the present research work was to fabricate aceclofenac loaded pectinate microspheres by ionic gelation method and evaluate the effect of different cross-linking agents and polymer concentration on particle size, encapsulation efficacy and drug release behavior. It was also investigated that whether this pectinate dosage form was able to target the drug release in intestinal region and prevent the different side effect associated with the drug in stomach or not. It was observed that particle size, encapsulation efficacy and in vitro drug release were largely depended on polymer concentration and cross-linking agents. It was also observed that pectinate microspheres showed excellent pH depended mucoadhesive properties and they were able to restrict the drug release in stomach. <em>In vitro</em> drug release study showed that alminium-pectinate microspheres have more sustaining property as compared to barium-pectinate microspheres. Holm-Sidak multiple comparison analysis suggested a significant difference in measured t<sub>50%</sub> values among all the formulations with same cross-linking agent. In vivo studies revealed that the anti inflammatory and analgesic effects induced by pectinate microspheres were significantly high and prolonged as compared to pure drug. So, pectinate microspheres can be an excellent carrier for targeting the delivery of aceclofenac as well as help in improving the patient compliance by prolonging the systemic absorption.

scholarly journals Formulation, Optimization, and Characterization of Repaglinide Loaded Nanocrystal for Diabetes Therapy

2015 ◽  
Vol 2015 ◽  
pp. 1-7 ◽  
Author(s):  
Gajanan Shinde ◽  
Mitesh Patel ◽  
Manan Mehta ◽  
Rajesh Kesarla ◽  
Ganesh Bangale
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Zeta Potential ◽  
Polymer Concentration ◽  
Study Data ◽  
Stability Study ◽  
Diabetes Therapy ◽  
Peg 4000 ◽  
Number Of Cycles

The aim of the present investigation was to formulate and characterize nanocrystal formulation of Repaglinide for diabetes therapy. Formulation was done by high pressure homogenization. HPH pressure and cycles range were screened by preliminary batches (T1 and T2). 5, 8, and 10 cycles and 500 to 1500 bar pressure range had kept for further investigation. Taguchi design was used to optimize type of polymer, % polymer concentration, number of cycles, and HPH pressure for nanocrystal formulation. Formulations were characterized for particle size, zeta potential, and in vitro drug release. Optimized formulation (NC 3) showed particle size of 187 nm, zeta potential of −29.4 mv, and % drug release of 80.58% and it was used for further study. Data analysis proved significant effects of factors on responses. Polydispersity index (PDI) Analysis of optimized formulation were found to be 0.248. SEM showed nanocrystal aggregation of drug, may be due to water removal process. DSC showed slight change in crystallinity, may be due to the presence of PEG 4000. Stability study was carried out for 3 months. It indicated no significant change in particle size and zeta potential. However, further studies in higher animals and human being need to be performed before this formulation can be commercially exploited.

scholarly journals Physicochemical Properties andIn VitroCytotoxicity Studies of Chitosan as a Potential Carrier for Dicer-Substrate siRNA

2013 ◽  
Vol 2013 ◽  
pp. 1-10 ◽  
Author(s):  
Maria Abdul Ghafoor Raja ◽  
Haliza Katas ◽  
Zariyantey Abd Hamid ◽  
Nur Atiqah Razali
Keyword(s):  
Particle Size ◽  
Cost Effectiveness ◽  
Zeta Potential ◽  
Small Interfering Rna ◽  
Ionic Gelation ◽  
Rapid Degradation ◽  
The Mean ◽  
Afm Micrographs ◽  
Interfering Rna

Recently, Dicer-substrate small interfering RNA (DsiRNA) has gained attention owing to its greater potency over small interfering RNA (siRNA). However, the use of DsiRNA is restricted by its rapid degradationin vitro. To address this issue, chitosan nanoparticulate deliver yplatform for the Dicer-substrate siRNA (DsiRNA) was developed and characterized. Nanoparticles were prepared by simple complexation and ionic gelation methods. The mean particle size of DsiRNA-adsorbed chitosan nanospheres (DsiRNA-CS NPs) prepared by the ionic gelation method ranged from 225 to 335 nm, while simple complexation yielded DsiRNA-chitosan complexes (DsiRNA-CS complexes) ranging from 270 to 730 nm. The zeta potential of both types of nanoparticles ranged from +40 to +65 mV. TEM and AFM micrographs revealed spherical and irregular morphology of DsiRNA-CS NPs and DsiRNA-CS complexes. ATR-FTIR spectroscopy confirmed the presence of DsiRNA in the CS NPs/complexes. Both types of nanoparticles exhibited sustained release and high binding and encapsulation (100%) efficiency of DsiRNA. DsiRNA-CS NPs/complexes showed low, concentration-dependent cytotoxicityin vitro. DsiRNA-CS NPs showed better stability than the complexes when stored at 4 and 25°C. Thus, it is anticipated that CS NPs are promising vectors for DsiRNA delivery due to their stability, safety, and cost-effectiveness.

scholarly journals Formulation and Evaluation of Acyclovir Microspheres

2018 ◽  
Vol 27 (1) ◽  
pp. 1-7
Author(s):  
Pavani S ◽  
Mounika K ◽  
Naresh K
Keyword(s):  
Particle Size ◽  
Sustained Release ◽  
Sodium Alginate ◽  
Calcium Chloride ◽  
Polymer Concentration ◽  
Entrapment Efficiency ◽  
In Vitro Dissolution ◽  
Release Mechanism ◽  
Natural Polymers

The present study is to formulate and evaluate Acyclovir (ACV) microspheres using natural polymers like chitosan and sodium alginate. ACV is a DNA polymerase inhibitor used in treating herpes simplex virus infection and zoster varicella infections. Acyclovir is a suitable candidate for sustained-release (SR) administration as a result of its dosage regimen twice or thrice a day and relatively short plasma half-life (approximately 2 to 4 hours). Microspheres of ACV were prepared by an ionic dilution method using chitosan and sodium alginate as polymers. The prepared ACV microspheres were then subjected to FTIR, SEM, particle size, % yield, entrapment efficiency, in vitro dissolution studies and release kinetics mechanism. The FTIR spectra’s revealed that, there was no interaction between polymer and ACV. ACV microspheres were spherical in nature, which was confirmed by SEM. The particle size of microspheres was in the range of 23.8µm to 39.4µm. 72.9% drug entrapment efficiency was obtained in the formulation F3 (1:3 ratio) with a high concentration of calcium chloride (4% w/v). The in vitro performance of ACV microspheres showed sustained release depending on the polymer concentration and concentration of calcium chloride.   The release data was best fitted with zero order kinetics and Korsemeyer -Peppas release mechanism and diffusion exponent ‘n’ value of was found to be Non-Fickian.

scholarly journals Development and Evaluation of Floating Microspheres of Sumatriptan Succinate using Ethyl Cellulose and Mucilage Extracted from Vigna Mungo

2021 ◽  
pp. 24-36
Author(s):  
Nilesh S. Kulkarni ◽  
Mukta A. Kulkarni ◽  
Rahul H. Khiste ◽  
Mohini C. Upadhye ◽  
Shashikant N. Dhole
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Ethyl Cellulose ◽  
Polymer Concentration ◽  
Average Particle Size ◽  
Entrapment Efficiency ◽  
Vigna Mungo ◽  
Average Particle ◽  
Sumatriptan Succinate

Aim: The present investigation is to formulate and evaluate gastroretentive floating microspheres for sumatriptan succinate. Gastric retention is widely used approach to retain dosage form in stomach and to enhance absorption of drugs. Methods: The gastroretentive floating microspheres was prepared by two different techniques as solvent evaporation and W/O/W multiple emulsion technique. Ethyl cellulose, HPMC K4M polymer and mucilage extracted from Vigna Mungo in various proportions were used for formulation of microspheres. Combination of ethyl acetate and acetone in different proportion was used as organic phase and the microspheres were characterized for particle size, shape, morphology, percentage yield, entrapment efficiency, drug loading, In-Vitro Floating/Buoyancy study, In-vitro Floating/Buoyancy study and release kinetics. Results: The average particle size of all batches was found in the range 100 to 210 μm and the entrapment efficiency of all formulations was found in the range of 17.46 % to 59.28 %.Total floating time for Sumatriptan succinate floating microspheres was observed more than 12 h. The In-Vitro drug release study was performed for all formulations showed drug release in controlled manner. Conclusion: The particle size was increased with increased polymer concentration and it showed that polymer concentration has an impact on the entrapment efficiency. Ethyl cellulose microspheres showed more entrapment and sustained delivery of sumatriptan Succinate than microspheres prepared by combination of Ethyl cellulose: HPMC K4M and Ethyl cellulose: Vigna mungo mucilage.

scholarly journals Chitosan-Based Polyelectrolyte Complexes for Doxorubicin and Zoledronic Acid Combined Therapy to Overcome Multidrug Resistance

Pharmaceutics ◽  
2018 ◽  
Vol 10 (4) ◽  
pp. 180 ◽  
Author(s):  
Simona Giarra ◽  
Silvia Zappavigna ◽  
Virginia Campani ◽  
Marianna Abate ◽  
Alessia Cossu ◽  
...  
Keyword(s):  
Zoledronic Acid ◽  
Cell Lines ◽  
Combined Therapy ◽  
Polymer Concentration ◽  
Resistant Cell ◽  
Wild Type ◽  
Polyelectrolyte Complexes ◽  
Ionotropic Gelation ◽  
Experimental Parameters

This study aimed to develop nanovectors co-encapsulating doxorubicin (Doxo) and zoledronic acid (Zol) for a combined therapy against Doxo-resistant tumors. Chitosan (CHI)-based polyelectrolyte complexes (PECs) prepared by ionotropic gelation technique were proposed. The influence of some experimental parameters was evaluated in order to optimize the PECs in terms of size and polydispersity index (PI). PEC stability was studied by monitoring size and zeta potential over time. In vitro studies were carried out on wild-type and Doxo-resistant cell lines, to assess both the synergism between Doxo and Zol, as well as the restoring of Doxo sensitivity. Polymer concentration, incubation time, and use of a surfactant were found to be crucial to achieving small size and monodisperse PECs. Doxo and Zol, only when encapsulated in PECs, showed a synergistic antiproliferative effect in all the tested cell lines. Importantly, the incubation of Doxo-resistant cell lines with Doxo/Zol co-encapsulating PECs resulted in the restoration of Doxo sensitivity.

scholarly journals Consequence of ANASTROZOLE on Chemo therapy

2017 ◽  
Vol 1 (2) ◽  
pp. 01-04
Author(s):  
Saritha Garrepalli
Keyword(s):  
Particle Size ◽  
In Vitro Release ◽  
Scanning Calorimetry ◽  
Ir Studies ◽  
Release Studies ◽  
Ft Ir ◽  
The Mean ◽  
Pure Drug ◽  
The Stability

Prepared nanoparticles were characterized in terms of particle size, scanning electron microscope (SEM), fourier transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC). In-vitro release studies were performed in phosphate buffer saline pH 7.4 at 37˚±0.5˚C for 1month. The mean particle size of obtained nanoparticles was 150-400 nm and was apparently spherical in shape, with smooth surface. DSC is done for the stability test for pure drug and sample. The thermogram of drug has not shifted for in the formulation compare to pure drug thermogram hence, the stability of formulation is not changed. FT-IR studies demonstrated that the drug was not changed in the formulation during the fabrication process.The encapsulation efficiency was about 48%. The Anastrozole-BSA nanoparticles exhibit a most interesting release profile with small initial burst followed by slower and controlled release.

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