Biodegradable microparticulate system of captopril

Dandagi, Panchaxari Mallappa; Mastiholimath, Vinayak; Patil, Manjusha; Gupta, Manish Kumar

doi:10.1016/j.ijpharm.2005.10.025

Cited by 30 publications

(23 citation statements)

References 9 publications

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“…Cottonseed oil was purchased from Acros organics (New Jersey, USA). (Dandagi et al, 2006;Kristina et al, 2001;Tuncay et al, 2000;Arshady, 1990) Table I represents the design of various formulations developed. BSA microparticles containing diltiazem HCl were prepared by emulsification-heat stabilization technique (Figure 1: show the systemic diagram of emulsification-heat stabilization technique).…”

Section: Methodsmentioning

confidence: 99%

“…Entrapment efficiency: (Dandagi et al, 2006;Yeo et al, 2004;Thakkar et al, 2005;Gupta et al, 2009) · Unentrapped drug: Ten milliliter of pH 7.4 phosphate buffer saline (PBS) was added to 10 mg of microparticles and this mixture was kept in an ultrasonicator for 1 minute. After centrifugation, the supernatant was filtered through a 0.45 μm filter and the filtrate was suitably diluted with buffer solution.…”

Section: Characterization Of Microparticlesmentioning

confidence: 99%

“…Particle size distribution and morphology of microparticles (Mathew et al, 2007;Dandagi et al, 2006;Yeo et al, 2004;Gupta et al, 2009) Size and morphology (shape and surface characteristics) were characterized by scanning electron microscopy using JEOL-T330A scanning microscope (Japan). Dry microparticles were placed on an electron microscope brass stub and coated with gold in an ion sputter.…”

Section: Drug Entrapment Efficiency = (M Actual / M Theoretical ) X 100%mentioning

confidence: 99%

“…In vivo drug distribution studies (Dandagi et al, 2006;Gupta et al, 2009;Oner et al,1993;Shenoy et al, 1997) This study was carried out to compare the targeting efficiency of drug-loaded microparticles and controlled release with that of the free drug in terms of percentage increase in targeting to various organs of reticule endothelial system like liver, lungs, kidney and spleen.…”

Section: Drug Entrapment Efficiency = (M Actual / M Theoretical ) X 100%mentioning

confidence: 99%

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Biodegradable microparticulate drug delivery system of diltiazem HCl

Gupta¹,

Prakash²,

Mishra

2012

Braz. J. Pharm. Sci.

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The efficacy of a drug in a specific application requires the maintenance of appropriate drug blood level concentration during a prolonged period of time. Controlled release delivery is available for many routes of administration and offers many advantages (as microparticles and nanoparticles) over immediate release delivery. These advantages include reduced dosing frequency, better therapeutic control, fewer side effects, and, consequently, these dosage forms are well accepted by patients. Advances in polymer material science, particle engineering design, manufacture, and nanotechnology have led the way to the introduction of several marketed controlled release products and several more are in pre-clinical and clinical development. The objective of this work is to prepare and evaluate diltiazem HCl loaded albumin microparticles using a factorial design. Albumin (natural polymer) microparticles were prepared by emulsion heat-stabilization method. Selected formulations were characterized for their entrapment efficiency, particle size, surface morphology, and release behavior. Analysis of variance for entrapment efficiency indicates that entrapment efficiency is best fitted to a response surface linear model. Surface morphology was studied by scanning electron microscopy. Scanning electron microscopy of the microparticles revealed a spherical, nonporous and uniform appearance, with a smooth surface. The geometric mean diameter of the microparticles was found to be 2-9 μm, which more than 75% were below 3.5 μm and drug incorporation efficiency of 59.74 to 72.48% (w/w). In vitro release profile for formulations containing diltiazem HCl loaded BSA microparticles with heat stabilization technique shows slow controlled the release of the drug up to 24 hours. The release pattern was biphasic, characterized by an initial burst effect followed by a slow release. All selected microparticles exhibited a prolonged release for almost 24 hours. On comparing regression-coefficient (r 2 ) values for Hixson Crowel, Higuchi and Peppas kinetic models, different batches of microparticles showed Fickian, non-Fickian, and diffusion kinetics. The release mechanism was regulated by D:P ratio. From the statistical analysis it was observed that as the drug:polymer (D:P) ratio increased, there was a significant increase in the encapsulation efficiency. Based on the particle size, entrapment efficiency and physical appearance, DTM-3 formulations were selected for in vivo release study and stability study. The in vivo result of drug loaded microparticles showed preferential drug targeting to liver followed by lungs, kidneys and spleen. Stability studies showed that maximum drug content and closest in vitro release to initial data were found in the formulation stored at 4 ºC. In present study, diltiazem HCl loaded BSA microparticles were prepared and targeted to various organs to satisfactory level and were found to be stable at 4 ºC.Uniterms: Diltiazem HCl loaded microparticles/preparation. Diltiazem HCl loaded microparticles/ release profil...

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Section: Methodsmentioning

confidence: 99%

Section: Characterization Of Microparticlesmentioning

confidence: 99%

Section: Drug Entrapment Efficiency = (M Actual / M Theoretical ) X 100%mentioning

confidence: 99%

Section: Drug Entrapment Efficiency = (M Actual / M Theoretical ) X 100%mentioning

confidence: 99%

See 2 more Smart Citations

Biodegradable microparticulate drug delivery system of diltiazem HCl

Gupta¹,

Prakash²,

Mishra

2012

Braz. J. Pharm. Sci.

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show abstract

“…[5][6][7] Water is a good solvent for such polymers during the preparation processes. In most cases, cross-linking agents are used to ensure particle generation.…”

Section: )mentioning

confidence: 99%

A Novel Preparation Method for Microspheres of Water Soluble Polymers Using Polypropyleneglycol as the Dispersion Medium

Seki

Shinohara

Kato

et al. 2007

CHEMICAL & PHARMACEUTICAL BULLETIN

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Microspheres (MS) are useful as drug carriers to improve the performance of therapeutic systems. For example, stable release by a valve and guaranteed delivery to the lung by a metered dose inhaler or dry powder inhaler formulations can be achieved using size-controlled spherical MS, 1) and the therapeutic drugs entrapped in MS and, when injected vascularly, can distribute to specific organs or tissues depending on their size. 2,3) The choice of the matrix material and size control of the MS are the most important factors in designing any therapeutic system. Lipophilic polymer esters such as poly(lactic-co-glycolic acid) are popular materials and exhibit prolonged drug release. On the other hand, hydrophilic polymers can be used for controlled release over shorter periods and may be better at entrapping MS for water-soluble drugs compared with lipophilic polymers. 4)MS consisting of hydrophilic polymers, such as proteins and polysaccharides, can be prepared by emulsion-evaporation and spray-drying. [5][6][7] Water is a good solvent for such polymers during the preparation processes. In most cases, cross-linking agents are used to ensure particle generation. 8)However, heating to evaporate water and addition of crosslinking agents may not be good for the stability of therapeutic drugs in MS.9,10) Although gelatin MS can be prepared in cooling processes to promote gel formation, cross-linking agents such as glutaraldehyde are needed to control drug release from the resulting MS.11) A novel preparation method for MS consisting of water soluble polymers, which can be applied to various types of polymers and does not require heating and cross-linking reactions during the preparation process, will be useful for the preparation of MS containing sensitive materials, such as protein drugs.In the present study, polypropyleneglycol (PPG) was used as a dispersion medium for the preparation of MS consisting of water-soluble polymers. PPG is hydrophobic at high temperatures but hydrophilic and freely soluble in water at low temperatures. Therefore, the PPG-water system forms two liquid phases like an emulsion at a high temperature and the system changes to a liquid phase on cooling. This temperature-dependent property of PPG can be used to remove water from aqueous polymer solutions dispersed in PPG to form solid polymer particles. Soluble starch is used mainly as the model water-soluble polymer. Gelatin, whey protein and dextran have also been used for MS preparation. ExperimentalMaterials Polypropyleneglycol (diol type 700, PPG) and soluble starch were purchased from Wako Pure Chemical (Osaka). Whey protein isolate (WPI) was kindly supplied by Snow Brand Milk Products (Tokyo). Dextran T70 and gelatin were purchased from Pharmacia Biotech (Uppsala, Sweden) and Nitta Gelatin (Osaka), respectively. All other chemicals were of reagent grade and used as received.Procedure for Microsphere Preparation Water soluble polymers (starch, gelatin, WPI or dextran T70) were initially dissolved in water (5-10%) at 60°C for the aqueous phas...

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Paromomycin‐loaded albumin microspheres: Efficacy and stability studies

Khan

Kumar

Singh

et al. 2012

Drug Testing and Analysis

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In the present work, paromomycin-loaded albumin microspheres (PM-MS) have been formulated for passive targeting of paromomycin (PM) to macrophages, for the treatment of visceral leishmaniasis (VL). PM-MS were prepared by spray-drying method with a mean particle size of ≈ 3 µm. Thermal and chemical cross-linking methods were used for controlling drug release from the prepared microspheres (MS). PM-MS were then tested for efficacy and stability studies. In efficacy study, in vitro promastigote assay was carried out to assess the susceptibility of promastigote to PM in the concentration range of 5.0-150 µg/ml; cytotoxicity assay was performed to determine possible toxicity of PM for the host cells (peritoneal macrophages) and intracellular amastigote assay was carried out to determine the efficacy of free PM (PM solution) and encapsulated PM (PM-MS). Results obtained indicated a significant increase in efficacy of PM-MS in comparison to PM solution at equivalent concentration. Subsequently, stability studies of prepared formulation was carried out at various temperature and humidity conditions, these studies provided stability of formulation at all tested conditions including accelerated conditions. Thus, it can be concluded that present work provides an optimized formulation with stability and enhanced efficacy.

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Biodegradable microparticulate system of captopril

Cited by 30 publications

References 9 publications

Biodegradable microparticulate drug delivery system of diltiazem HCl

Biodegradable microparticulate drug delivery system of diltiazem HCl

A Novel Preparation Method for Microspheres of Water Soluble Polymers Using Polypropyleneglycol as the Dispersion Medium

Paromomycin‐loaded albumin microspheres: Efficacy and stability studies

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