Biodegradable microspheres of poly(DL-lactic acid) containing piroxicam as a model drug for controlled release via the parenteral route

Lalla, J. K.; Sapna, K.

doi:10.3109/02652049309015322

Cited by 37 publications

(14 citation statements)

References 10 publications

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“…In previous studies, PLGA and Eudragit RL formed homogeneous nanostructures when examined by differential scanning calorimeter, X-ray diffractometer, and Fourier transform infrared spectroscopy 21–23. PLGA polymer and hydrophobic group of Eudragit RL (methacrylic acid derivatives) preferentially formed the inner core structure of the NPs, while the positively charged moiety of Eudragit RL (quaternary ammonium groups) was on the surface of the NPs.…”

Section: Resultsmentioning

confidence: 95%

Increased localized delivery of piroxicam by cationic nanoparticles after intra-articular injection

Kim¹,

Ho²,

Kim³

et al. 2016

DDDT

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Piroxicam (PRX), a potent nonsteroidal anti-inflammatory drug, is prescribed to relieve postoperative and/or chronic joint pain. However, its oral administration often results in serious gastrointestinal adverse effects including duodenal ulceration. Thus, a novel cationic nanoparticle (NP) was explored to minimize the systemic exposure and increase the retention time of PRX in the joint after intra-articular (IA) injection, by forming micrometer-sized electrostatic clusters with endogenous hyaluronic acid (HA) in the synovial cavity. PRX-loaded NPs consisting of poly(lactic-co-glycolic acid), Eudragit RL, and polyvinyl alcohol were constructed with the following characteristics: particle size of 220 nm, zeta potential of 11.5 mV in phosphate-buffered saline, and loading amount of 4.0% (w/w) of PRX. In optical and hyperspectral observations, the cationic NPs formed more than 50 μm-sized aggregates with HA, which was larger than the intercellular gaps between synoviocytes. In an in vivo pharmacokinetic study in rats, area under the plasma concentration–time curve (AUC0–24 h) and maximum plasma concentration (Cmax) of PRX after IA injection of the cationic NPs were <70% (P<0.05) and 60% (P<0.05), respectively, compared to those obtained from drug solution. Moreover, the drug concentration in joint tissue 24 h after dosing with the cationic NPs was 3.2-fold (P<0.05) and 1.8-fold (P<0.05) higher than that from drug solution and neutrally charged NPs, respectively. Therefore, we recommend the IA cationic NP therapy as an effective alternative to traditional oral therapy with PRX, as it increases drug retention selectively in the joint.

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Section: Resultsmentioning

confidence: 95%

Increased localized delivery of piroxicam by cationic nanoparticles after intra-articular injection

Kim¹,

Ho²,

Kim³

et al. 2016

DDDT

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“…6) In this study the lipophilic drugs were made aqueous soluble by dissolving in a mixture containing ethanol and water then further proceeded with multiple emulsion solvent evaporation method, the method is most successful with drugs which are insoluble or poorly soluble in aqueous medium. 8,9) Many types of drugs with different physical and chemical properties have been formulated into polymeric systems, including anti cancer drugs, 10,11) narcotic agents, 12,13) local anaesthetics, 14) steroids 15,16) and fertility control agents 17,18) using solvent evaporation method of microencapsulation.…”

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confidence: 99%

Influence of Manufacturing Parameters on Development of Contraceptive Steroid Loaded Injectable Microspheres

2004

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The main objective of this work was to develop a system consisting of polymeric microspheres loaded with steroid drugs. The drugs were encapsulated using biodegradable poly(lactide-co-glycolide) (PLG) and poly(e ecaprolactone) (PCL) by double emulsion solvent evaporation method. The lipophilic drugs, levonorgestrel and ethinylestradiol were made soluble by adding ethanol/water mixture. The effects of parameters like polymer concentration and stabilizer concentration were studied on the size, size distribution, surface properties and loading efficiencies of microspheres. The formulated microspheres were smooth, spherical and uniform in shape and size. Fourier transformed infrared spectroscopy and differential scanning calorimetry studies seemed to confirm the absence of chemical interaction between the drugs and the polymers, while the drugs were dispersed in the polymer. The increase in polymer concentrations increased the size as well as the loading efficiency of microspheres. Data obtained in this study demonstrated that the PLG/PCL microspheres may be a suitable polymeric carrier for long acting injectable drug delivery.

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“…Also, HPMC (Gursoy and Cevik 2000) and gelatin (Chowdhury and Mitra 2000), which are viscosity-increasing agents, have been widely used in ophthalmic preparations, and vitamin E in the treatment of ophthalmic diseases (Brayfield 1999). In its turn, PEG was used as a channelling agent to improve the release rate of certain drugs from microspheres (Lalla and Sapna 1993, Khidr et al 1998, Mallard et al 2000a, isopropyl myristate to modify the release profiles of several drugs (Juni et al 1985, Wang et al 1996, and Labrafil Õ M 1944 CS, a nonionic excipient, a widely used solubilizer and dispersing vehicle for pharmaceutical products (Gao et al 1995).…”

Section: Introductionmentioning

confidence: 99%

Poly (D,L-lactide-co-glycolide) microspheres for long-term intravitreal delivery of aciclovir: influence of fatty and non-fatty additives

Martínez-Sancho

Herrero-Vanrell

Negro

2003

Journal of Microencapsulation

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Aciclovir (acicloguanosine) has been demonstrated to be effective in the treatment of intraocular pathologies such as herpes simplex virus retinitis and acute retinal necrosis. Although intravitreal injections have been used with fewer side-effects than intravenous administration, the risk of complications increases with the frequency of intravitreous injections. For this reason, a biodegradable drug-delivery system, such as microspheres, able to promote prolonged release of the drug, offers a good alternative to multiple intraocular administrations. In this work, aciclovir-containing poly (D,L-lactide-co-glycolide) microspheres were prepared by the solvent evaporation method. Seven additives were incorporated in the microspheres to modulate the in vitro release rate of the drug: four non-fatty substances (polyethylene glycol 300, polyethylene glycol 1500, hydroxypropyl methylcellulose and gelatin) and three fatty substances (isopropyl myristate, vitamin E and Labrafil M 1944 CS). Morphology of microspheres was evaluated by scanning electron microscopy. Granulometric analysis showed that particle size distribution was significantly influenced by the incorporation of additives. Loading efficiency decreased when fatty substances were added, whereas non-fatty additives promoted higher incorporation of the drug. Infrared and differential scanning calorimetry analyses indicated that microspheres prepared by the solvent evaporation process were not influenced by the type of additive used. In all cases, the initial burst resulted less than 5%. Additive-free microspheres showed a slow release within the first days, but when additives were incorporated, in general, the release rates of the drug were increased. Best release results were obtained for gelatin-containing microspheres. The release of aciclovir from these microspheres was adjusted to a zero-order kinetic from 1 to 49 days with a release constant of 1.13 microg/day/mg microspheres. A dose of 0.74 mg microspheres would be therapeutic for the herpes simplex and Epstein-Barr viruses (MIC 0.1 microg/ml) and 7.4 mg for varicella zoster virus (MIC 1 microg/ml) treatment in an animal model.

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Biodegradable microspheres of poly(DL-lactic acid) containing piroxicam as a model drug for controlled release via the parenteral route

Cited by 37 publications

References 10 publications

Increased localized delivery of piroxicam by cationic nanoparticles after intra-articular injection

Increased localized delivery of piroxicam by cationic nanoparticles after intra-articular injection

Influence of Manufacturing Parameters on Development of Contraceptive Steroid Loaded Injectable Microspheres

Poly (D,L-lactide-co-glycolide) microspheres for long-term intravitreal delivery of aciclovir: influence of fatty and non-fatty additives

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