scholarly journals Risperidone Controlled Release Microspheres Based on Poly(Lactic Acid)-Poly(Propylene Adipate) Novel Polymer Blends Appropriate for Long Acting Injectable Formulations

Pharmaceutics ◽  
2018 ◽  
Vol 10 (3) ◽  
pp. 130 ◽  
Author(s):  
Stavroula Nanaki ◽  
Panagiotis Barmpalexis ◽  
Alexandros Iatrou ◽  
Evi Christodoulou ◽  
Margaritis Kostoglou ◽  
...  
Keyword(s):  
Lactic Acid ◽  
Controlled Release ◽  
Drug Release ◽  
Polymer Blends ◽  
Solvent Evaporation ◽  
Poly Lactic Acid ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Long Acting ◽  
Poly Propylene

The present study evaluates the preparation of risperidone controlled release microspheres as appropriate long-acting injectable formulations based on a series of novel biodegradable and biocompatible poly(lactic acid)–poly(propylene adipate) (PLA/PPAd) polymer blends. Initially, PPAd was synthesized using a two-stage melt polycondensation method (esterification and polycondensation) and characterized by 1H-NMR, differential scanning calorimetry (DSC), and powder X-ray diffraction (XRD) analyses. DSC and XRD results for PLA/PPAd blends (prepared by the solvent evaporation method) showed that these are immiscible, while enzymatic hydrolysis studies performed at 37 °C showed increased mass loss for PPAd compared to PLA. Risperidone-polyester microparticles prepared by the oil–water emulsification/solvent evaporation method showed smooth spherical surface with particle sizes from 1 to 15 μm. DSC, XRD, and Fourier-transformed infrared (FTIR) analyses showed that the active pharmaceutical ingredient (API) was dispersed in the amorphous phase within the polymer matrices, whereas in vitro drug release studies showed risperidone controlled release rates in all PLA/PPAd blend formulations. Finally, statistical moment analysis showed that polyester hydrolysis had a major impact on API release kinetics, while in PLA/PPAd blends with high PLA content, drug release was mainly controlled by diffusion.

Synthesis and Kinetic Studies on Controlled Release of 6-Thioguanine Entrapped Polyethylene Glycol-Co-Polylactic Acid Polymer Nanoparticles

2011 ◽  
Vol 9 (1) ◽  
Author(s):  
Sathishkumar Kannaiyan ◽  
T.G.Ashwin Narayanan ◽  
P.Karthick Sarathy ◽  
Nagarjun Sudhakar ◽  
Rama Krishnan
Keyword(s):  
Gold Nanoparticles ◽  
Lactic Acid ◽  
Polyethylene Glycol ◽  
Controlled Release ◽  
Drug Release ◽  
Kinetic Equations ◽  
Kinetic Studies ◽  
Poly Lactic Acid ◽  
Average Size

Poly lactic acid-polyethylene glycol (PLA-co-PEG) copolyester was synthesized from oligomer of L-lactic acid and poly ethylene glycol (PEG) using stannous octoate as catalyst. 6-Thioguanine containing Poly lactic acid-polyethylene glycol (PLA-co-PEG) nanocapsules were prepared in the presence and absence of gold nanoparticles via the W/O/W emulsification solvent-evaporation method. The morphologies of prepared nanocapsules changed substantially because of the presence of gold nanoparticles. From SEM and TEM measurements, the average size of the polymer nanocapsules and gold nanoparticles were found to be in range of 230-260 nm and 18-20 nm, respectively. In general the drug release was quicker in Phosphate buffer saline (pH 7.4) compared to 0.1M hydrochloric acid and this may be due to higher solubility, higher swelling and penetration properties of PLA-co-PEG in PBS compared to HCl. Polymer nanocapsules with gold show a prolonged controlled release with higher encapsulation efficiency (75%) compared to that of polymer nanocapsules (45%) in the absence of gold nanoparticles. It may be due to the more entrapping efficiency of gold and less diffusivity of drugs from the nanocapsules. Application of in vitro drug release data to various kinetic equations indicated Higuchi model, indicating a uniform distribution of thioguanine in the nanocapsules.

scholarly journals FORMULATION AND EVALUATION OF FLOATING MICROSPHERES OF CIPROFLOXACIN BY SOLVENT EVAPORATION METHOD USING DIFFERENT POLYMERS

2021 ◽  
pp. 101-108
Author(s):  
KAUSLYA ARUMUGAM ◽  
PAYAL D. BORAWAKE ◽  
JITENDRA V. SHINDE
Keyword(s):  
Particle Size ◽  
Drug Release ◽  
Release Kinetics ◽  
Methyl Cellulose ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
Angle Of Repose ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Objective: The main intention of this research was to formulate and evaluate floating microspheres of ciprofloxacin using different polymers to prolong gastric residence time. Methods: The microspheres were formulated by the solvent evaporation method using different ratios of polymers like carbopol 940, ethylcellulose, and Hydroxy Propyl Methyl Cellulose K4M. Further, the floating microspheres were evaluated for micromeritic properties like bulk density, tapped density, angle of repose, etc., percentage yield, particle size, entrapment efficiency, floating capacity, in vitro drug release study, release kinetics, drug content, swelling index, and Fourier Transform Infrared Spectroscopy (FTIR) (Compatibility studies). Results: The ciprofloxacin microspheres showed the good flowing property. The particle size ranged from 258.1±2.21 µm to 278±2.86 µm and entrapment efficiency ranged from 63.17±0.43% to 89.90±1.32%. The IR spectrum revealed that there was no interaction between the drug and polymer. F7 formulation was found to be the best formulation. Drug release was found to be 90.70±0.89% i.e. in a controlled manner at the end of 10 h. Conclusion: The floating microspheres were prepared successfully and the results clearly stated that prepared ciprofloxacin microspheres may be safe and effective controlled drug delivery over an extended period which can increase bioavailability, patient compliance, and decrease dosing frequency.

Fabrication, characterization, and controlled release of eprinomectin from injectable mesoporous PLGA microspheres

RSC Advances ◽  
2015 ◽  
Vol 5 (92) ◽  
pp. 75025-75032 ◽  
Author(s):  
Qing Shang ◽  
Jianhua Zhai ◽  
Ruiqiong Tian ◽  
Ting Zheng ◽  
Xiaoyun Zhang ◽  
...  
Keyword(s):  
Controlled Release ◽  
Solvent Evaporation ◽  
Plga Microspheres ◽  
Solvent Evaporation Method ◽  
Evaporation Method

Batches of mesoporous poly(lactide-co-glycolide) (PLGA) microspheres were fabricated via an O/W emulsion–solvent evaporation method.

scholarly journals Formulation Development and Evaluation of Sustained Release Microsphere of Levetiracetam

2021 ◽  
Vol 71 (2) ◽  
Author(s):  
Dinesh V. Panpaliya ◽  
Atish Y. Sahare ◽  
Priyanka Lanje ◽  
Pooja Dhoke
Keyword(s):  
Drug Release ◽  
Entrapment Efficiency ◽  
Solvent Evaporation ◽  
In Vitro Dissolution ◽  
Compatibility Study ◽  
Solvent Evaporation Method ◽  
Formulation Development ◽  
Sustained Drug Release ◽  
Evaporation Method

The aim of the present work was to develop and evaluate of oral microsphere of Levetiracetam to reduce the frequency of dosing by achieving 12 hours sustained drug release. The microsphere formed will also mask the bitter taste of the drug and thus increase the compatibility of the drug with the patients. Levetiracetam is a second-generation anti-epileptic agent useful in the treatment of partial onset and monoclinic seizures. It has a short half life of 7 hours and its recommended dose is 500 mg twice a daily. Microspheres are suitable drug delivery system for such drug candidate. For these reasons it is must to formulate a suitable dosage form by which it will be easier to administer the dose and also to get a sustained drug release hence microsphere was prepared using solvent evaporation method. Preformulation studies were carried out to rule out any drug polymer interaction by FTIR technique. In this study formulation was done solvent evaporation method using different percentage of HPMC– K 100, HPMC- K 15 and coated with Eudragit S100. Drug, polymer and physical mixture were evaluated for in compatibility study by Fourier transforms infrared spectroscopy. All the batches of microsphere (F1 to F5) were subjected for in vitro dissolution. Microsphere was evaluated for surface morphology, micromeritics properties, entrapment efficiency and in vitro drug release. The entrapment efficiency of microsphere ranged from 71.16%-73.66%. The size of the prepared microsphere ranges between 42.8 µm to 55.64 µm which was found to increase with increase in RPM at same polymer ratio. Micromeritics studies showed good flow properties. Among the microsphere batches, F5 was observed as an optimized batch as its formulation with polymer i.e. Eudragit-S 100 and HPMC-K 100 was found to be release in sustained manner. The F-5 batch shows is 79.45% drug release at the end of 7 hrs and its stability study indicate that these microspheres were stable at selected temperature and humidity

scholarly journals Formulation and evaluation of floating microspheres of losartan potassium using sodium alginate and HPMC by solvent evaporation method

2019 ◽  
Vol 9 (1-s) ◽  
pp. 60-66 ◽  
Author(s):  
Kapil Purohit ◽  
Navneet Garud
Keyword(s):  
Drug Release ◽  
Solvent Evaporation ◽  
Losartan Potassium ◽  
Solvent Evaporation Method ◽  
In Vitro Drug Release ◽  
Evaporation Method ◽  
Sustained Action ◽  
Improve Patient

Hollow multі-unіt mіcrospheres were prepared by a solvent dіffusіon technіque іn emulsіon wіth a drug and an acrylіc polymer. These were dіssolved іn a mіxture of ethanol-dіchloromethane and poured іnto an aqueous solutіon of PVA wіth stіrrіng to form emulsіon droplets. The rate of drug release іn mіcro balloons was controlled by changіng the ratіo of polymer to drug. The mіcroballoons were floatіng іn vіtro for 12-24 hours when submerged іn aqueous medіa. Radіographіc studіes showed that mіcroballons admіnіstered orally to humans were dіspersed іn the upper part of the stomach and were held there for 3 hours agaіnst perіstaltіc movement. Floating Microspheres of Losartan potassium were formed by Solvent Evaporation method .The formulas LP7 of Losartan Potassium Floating Microspheres shows a very good drug release profiles and shown better sustained action till the end of last hour (24th hrs). It will improve patient compliance and increase in bioavailability which give better approach to treat hypertensive condition and the angiotensin receptor blocking action of Losartan lower the long term complications of Hypertension and reduce the risk of heart failure, CHF, Myocardial Infarction and also vascular damage in blood vessels and kidney. Keywords: Losartan Potassium, Floating microspheres, Drug Entrapment, In-vitro drug release.

scholarly journals Design and Development of Sustained Release Microspheres of Ibuprofen by Emulsification Solvent Evaporation Method Using Polymeric Blend

2013 ◽  
Vol 16 (1) ◽  
pp. 39-44 ◽  
Author(s):  
Nandini Saha ◽  
Ikramul Hasan ◽  
Mehrina Nazmi ◽  
Md Selim Reza
Keyword(s):  
Drug Release ◽  
Fourier Transforms ◽  
In Vitro Release ◽  
Pharmaceutical Journal ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Dissolution Apparatus ◽  
Emulsification Solvent Evaporation

Ibuprofen, a non-steroidal anti-inflammatory drug was formulated as microspheres by using Methocel K4M & Eudragit RSPO. These microspheres were prepared by emulsification solvent evaporation method to provide sustained action and to minimize local side effect of Ibuprofen by avoiding the drug release in the upper gastrointestinal tract. The prepared microspheres were subjected to various evaluation and in-vitro release studies. In-vitro drug release was studied in a paddle type dissolution apparatus (USP Type II Dissolution Apparatus) using Phosphate buffer (pH 7.4) as the dissolution medium at 37.5oC for 6 hours (paddle speed 50 RPM). The release mechanisms were explored and explained with Zero Order, First Order, Higuchi and Korsmeyer-Peppas equations. The correlation coefficients values of the trend lines of the graphs showed that the formulations best fit with Korsmeyer-Peppas release pattern. Microspheres’ morphology and chemical integrity were studied by a scanning electron microscope (SEM) and Fourier transforms infrared spectroscopy (FTIR) respectively. DOI: http://dx.doi.org/10.3329/bpj.v16i1.14489 Bangladesh Pharmaceutical Journal 16(1): 39-44, 2013

scholarly journals Evaluation of the Influence of Stirring Speed on the Release Kinetics of Fexofenadine HCl Polymeric Microspheres

2021 ◽  
Vol 18 (4) ◽  
pp. 733-741 ◽  
Author(s):  
Paroma Arefin ◽  
Md Shehan Habib ◽  
Mohammad Mostafa ◽  
Dipankar Chakraborty ◽  
Sreebash Chandra Bhattacharjee ◽  
...  
Keyword(s):  
Drug Release ◽  
Sustained Release ◽  
Release Kinetics ◽  
Drug Loading ◽  
Solvent Evaporation ◽  
Solvent Evaporation Method ◽  
Evaporation Method ◽  
Stirring Rate ◽  
The Impact ◽  
Fexofenadine Hcl

Microspheres, a potential drug delivery approach, has opened a new era for attaining versatile release patterns needed. By optimizing the formulation variables, they can be prepared to obtain targeted release, immediate release, sustained release patterns. The release of the active drug material depends upon a number of formulation parameters such as polymers, stirring speed (rpm), methodology, surfactants, etc. Fexofenadine hydrochloride (HCl) is a second generation antihistamine. Our present research has explored the effects of using different rpm (600- 1000 rpm) in preparing fexofenadine hydrochloride (HCl) microspheres by emulsion solvent evaporation method. The formulation is aimed to provide sustained release for the required long period with a high margin of safety. We used a blended mixture of Hydroxy Propyl Methyl Cellulose (HPMC) K 100 MCR and Eudragit RL100 polymers to have sustained-release microspheres. The impact of different rpm on Yield, drug encapsulation efficiency, flow properties, and dissolution pattern were appraised. We observed the release of the drug for 10 hours in phosphate buffer (pH 6.8) and evaluated the drug release spectrophotometrically. Our study finds that the release of fexofenadine HCl from the microspheres was significantly increased with drug loading. We found the dosage forms to follow Higuchi release kinetics and Hixson-Crowell release kinetics the most, indicating successful achievement of sustained-release pattern in the dosage form. The change in drug release rate was statistically significant for variation in the stirring rate. We found that 600 rpm was the most optimized stirring rate for preparing microspheres in the emulsion solvent evaporation method.

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