Controlled-release and antibacterial studies of doxycycline-loaded poly(ε-caprolactone) microspheres

Raval, Jignesh P.; Naik, Deep R.; Amin, Keyur A.; Patel, Paresh N.

doi:10.1016/j.jscs.2011.11.004

Cited by 44 publications

(26 citation statements)

References 21 publications

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“…Increasing the amount of polymer used resulted in an increase in the % EE due to an increase in the amount of polymer available for encapsulation of RIF and similar data has been reported [43][44][45][46]. The contribution of a high polymer content to the % EE can be interpreted in two ways, viz., (i) in highly concentrated solutions, the polymer precipitates more rapidly onto the surfaces of the dispersed phase and prevents API diffusion across the phase boundary [47] or (ii), the use of a high concentration of polymer results in an increase in the viscosity of the solution and delays API diffusion within the polymer droplets [48].…”

Section: Manufacture Of Isoniazid Microspheres Evaluation Of Model Asupporting

confidence: 61%

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Mwila

Walker

2020

Pharmaceutics

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The degradation of rifampicin (RIF) in an acidic medium to form 3-formyl rifamycin SV, a poorly absorbed compound, is accelerated in the presence of isoniazid, contributing to the poor bioavailability of rifampicin. This manuscript presents a novel approach in which isoniazid is formulated into gastric-resistant sustained-release microspheres and RIF into microporous floating sustained-release microspheres to reduce the potential for interaction between RIF and isoniazid (INH) in an acidic environment. Hydroxypropyl methylcellulose acetate succinate and Eudragit® L100 polymers were used for the manufacture of isoniazid-loaded gastric-resistant sustained-release microspheres using an o/o solvent emulsification evaporation approach. Microporous floating sustained-release microspheres for the delivery of rifampicin in the stomach were manufactured using emulsification and a diffusion/evaporation process. The design of experiments was used to evaluate the impact of input variables on predefined responses or quality attributes of the microspheres. The percent degradation of rifampicin following 12 h dissolution testing in 0.1 M HCl pH 1.2 in the presence of isoniazid gastric-resistant sustained-release microspheres was only 4.44%. These results indicate that the degradation of rifampicin in the presence of isoniazid in acidic media can be reduced by encapsulation of both active pharmaceutical ingredients to ensure release in different segments of the gastrointestinal tract, potentially improving the bioavailability of rifampicin.

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Section: Manufacture Of Isoniazid Microspheres Evaluation Of Model Asupporting

confidence: 61%

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Mwila

Walker

2020

Pharmaceutics

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“…Moreover, PCL is regarded as a green environmental and non-toxic polymer material due to its prominent biocompatibility and biodegradation. Thus, PCL is widely used in medical tissue engineering, drug delivery, and control release systems, food packaging industry, antibacterial study, protective clothing fabrication, and biosensors [4][5][6][7][8][9]. Particularly, micro-or nanoscale PCL particles with a wide specific surface area, a small pore size, high encapsulation efficiency, and a high porosity are considered to be the main candidates in these fields [10,11].…”

Section: Introductionmentioning

confidence: 99%

Influence of Solvent Selection in the Electrospraying Process of Polycaprolactone

2019

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Electrosprayed polycaprolactone (PCL) microparticles are widely used in medical tissueengineering, drug control release delivery, and food packaging due to their prominent structuresand properties. In electrospraying, the selection of a suitable solvent system as the carrier of PCL isfundamental and a prerequisite for the stabilization of electrospraying, and the control ofmorphology and structure of electrosprayed particles. The latter is not only critical for diversifyingthe characteristics of electrosprayed particles and achieving improvement in their properties, butalso promotes the efficiency of the process and deepens the applications of electrosprayed particlesin various fields. In order to make it systematic and more accessible, this review mainly concludesthe effects of different solution properties on the operating parameters in electrospraying on theformation of Taylor cone and the final structure as well as the morphology. Meanwhile,correlations between operating parameters and electrospraying stages are summarized as well.Finally, this review provides detailed guidance on the selection of a suitable solvent systemregarding the desired morphology, structure, and applications of PCL particles.

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“…NPH-MS were fabricated using double emulsion solvent evaporation technique ( Figure 2) [11,12]. Briefly, aqueous solution of NPH (1 part) was prepared in distilled water:acetone (1:1) mixture.…”

Section: Fabrication Of Nph-loaded Phb/pcl Biodegradable Microspheresmentioning

confidence: 99%

“…In-vitro drug release profiles from NPH, physical mixture and NPH-MS were studied in phosphate buffer (pH 7.4) using pretreated dialysis membrane (Himedia, India) having molecular weight cut-off (MWCO) of $12,000-14,000 Da [15]. Dialysis bag containing NPH-MS (equivalent to 180 mg NPH) was dipped in 100 mL of phosphate buffer (pH 7.4), and flask was placed in shaking incubator maintained at 100 rpm and 37 ± 0.5 C [12,16,17]. Samples were withdrawn periodically and reloaded with equivalent volume of dissolution medium.…”

Section: In-vitro Drug Release Studymentioning

confidence: 99%

Nefopam hydrochloride loaded microspheres for post-operative pain management: synthesis, physicochemical characterization and in-vivo evaluation

Sharma

Arora

Madan³

2017

Artificial Cells, Nanomedicine, and Biotechnology

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Once-daily oral dosage of nefopam hydrochloride loaded sustained release microspheres (NPH-MS) was investigated as novel therapeutic strategy for post-operative pain management. Microspheres were synthesized using poly-3-hydroxybutyrate and poly-(ɛ-caprolactone) by double emulsion solvent evaporation technique. NPH-MS were characterized through FTIR, PXRD and SEM. In-vitro drug release study revealed sustained behavior till 24 h. Haemolysis was <5% which signified haemocompatibility of formulation. ED50 in rat tail-flick anti-nociceptive test was found ∼18.12 mg/kg. In post-operative pain model, reversal of mechanical allodynia and thermal hyperalgesia by NPH-MS was statistically significant (p < .001) as compared with NPH till 24 h post-dose.

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Controlled-release and antibacterial studies of doxycycline-loaded poly(ε-caprolactone) microspheres

Cited by 44 publications

References 21 publications

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Improved Stability of Rifampicin in the Presence of Gastric-Resistant Isoniazid Microspheres in Acidic Media

Influence of Solvent Selection in the Electrospraying Process of Polycaprolactone

Nefopam hydrochloride loaded microspheres for post-operative pain management: synthesis, physicochemical characterization and in-vivo evaluation

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