[8] Poly(lactide-co-glycolide) microcapsules for controlled release of steroids

Cowsar, Donald R.; Tice, Thomas R.; Gilley, Richard M.; English, James P.

doi:10.1016/s0076-6879(85)12010-0

Cited by 85 publications

(33 citation statements)

References 4 publications

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“…Microspheres have been used for sustained drug release [11][12][13][14][15][16][17]. Polylactic acid microspheres have been studied extensively in other systems [11][12][13][14][15][16][17]. They are biodegradable to nontoxic compounds and have been demonstrated to incorporate readily lipid soluble drugs [11][12].…”

Section: Introductionmentioning

confidence: 99%

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Sustained local drug delivery to the arterial wall via biodegradable microspheres

Dev¹,

Eigler²,

Fishbein

et al. 1997

Cathet. Cardiovasc. Diagn.

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Section: Introductionmentioning

confidence: 99%

“…They are biodegradable to nontoxic compounds and have been demonstrated to incorporate readily lipid soluble drugs [11][12]. The rate of drug release can be varied by altering the size and drug content of the microspheres and degree of polymer cross linking [13][14].…”

Section: Introductionmentioning

confidence: 99%

Sustained local drug delivery to the arterial wall via biodegradable microspheres

Dev¹,

Eigler²,

Fishbein

et al. 1997

Cathet. Cardiovasc. Diagn.

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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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“…As discussed in our previous publications, the microsphere formulations used in these studies are known to be biocompatible (26,27,28) and capable of degradation to lactic and glycolic acids by nonenzymatic reactions (24). This technology has been used for sustained delivery of various biological components, including antigens, steroids, peptides, proteins, and antibiotics (1,3,9,10,11,12,14,15,21,23,25).…”

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confidence: 99%

Treatment of Tuberculosis Using a Combination of Sustained-Release Rifampin-Loaded Microspheres and Oral Dosing with Isoniazid

Quenelle¹,

Winchester²,

Staas³

et al. 2001

Antimicrob Agents Chemother

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Previously, we reported on the use of rifampin-loaded microspheres to effectively treat Mycobacterium tuberculosis-infected macrophages and mice. Using similar biocompatible polymeric excipients of lactide and glycolide copolymers, we have increased the rifampin loading of small microsphere formulations (1 to 10 m) by fourfold. Improved formulations were evaluated individually and in combination with oral regimens of isoniazid for the treatment of Mycobacterium tuberculosis H37Rv-infected mice. Groups (10 mice per group) consisted of mice that received (i) oral dosages of isoniazid (25 to 0.19 mg/kg of body weight/day), (ii) two intraperitoneal injections of rifampin-loaded microspheres on days 0 and 7, (iii) a combination of small rifampin-loaded microspheres on days 0 and 7 and isoniazid orally for 25 days (12.5 to 0.39 mg/kg/day), (iv) placebo injections, and (v) no treatment. Treatment with rifampin-loaded microspheres alone resulted in significant reductions in the numbers of CFU in the lungs and spleens by day 26. A bioassay revealed that plasma rifampin levels from the microspheres exceeded the MICs by more than twofold throughout the 26-day experimental period. Susceptibility testing demonstrated continued sensitivity to rifampin during the treatment period. Whereas isoniazid alone significantly reduced the numbers of CFU for dosages ranging from 12.5 to 1.56 mg/kg, combination therapy with rifampin-loaded microspheres increased the effective range to 0.39 mg/kg. In many cases, complete elimination of CFU was obtained with the combination therapy, something not achieved with most of the single therapies. These results demonstrate the ability to use small microsphere formulations alone to achieve significant results in a murine tuberculosis model and also the ability to use them safely in combination with another antimycobacterial agent.

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[8] Poly(lactide-co-glycolide) microcapsules for controlled release of steroids

Cited by 85 publications

References 4 publications

Sustained local drug delivery to the arterial wall via biodegradable microspheres

Sustained local drug delivery to the arterial wall via biodegradable microspheres

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

Treatment of Tuberculosis Using a Combination of Sustained-Release Rifampin-Loaded Microspheres and Oral Dosing with Isoniazid

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