In vitro and in vivo evaluation of taxol release from poly(lactic-co-glycolic acid) microspheres containing isopropyl myristate and degradation of the microspheres

Wang, Ya Min; Sato, Hitoshi; Horikoshi, Isamu

doi:10.1016/s0168-3659(97)00082-5

Cited by 56 publications

(18 citation statements)

References 24 publications

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“…A series of in vitro dissolution experiments were conducted using phosphate buffer at various pHs such as at 1.2, 6.8, and distilled water at 37 ± 2 ºC for 24 h. It was observed that the release behavior of CVD from the polymeric matrix of CVD-loaded EC-NPs, PEG-NPs, and PLGA-PEG-NPs exhibited biphasic pattern characterized by a fast initial release during the first 10 min followed by a slower and continuous release of drug as shown in Fig.6 (A1). Similar release pattern has also been previously observed from other PLGA polymeric systems 26,27 . The burst release of drugs might be due to the dissolution and diffusion of the drug that was poorly entrapped in the polymer matrix, while the slower and continuous release may be attributed to the diffusion of the drug localised in the EC-/PEG-/PLGA-PEG-core of the NPs.…”

Section: In Vitro Release Profilesupporting

confidence: 88%

Untitled

2016

IJPSR

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Nanoparticles (NPs) have been extensively studied during the past few decades due to their well-recognised applicability. Thus, the present study was aimed to fabricate Carvedilol (CVD) a β-adrenoceptor antagonist, as NPs aiming towards the optimal physicochemical characteristics and improved solubility. The prepared NPs demonstrated a linear increase in the mean particle size from253 ± 19 to 598 ± 21 nm and entrapment efficiency (%EE) from 58.6% to 91.1%, when drug-to-polymer mass ratio was increased from 1:1 to 1:5. In vitro release studies showed significant variation in the rate and extent of CVD release from polymeric matrix at various pHs of release media (pH 1.2, pH 6.8 and distilled water) and drug-to-polymer mass ratios. The present study highlighted the optimal formulation conditions to fabricate CVD-loaded NPs with best physicochemical characteristics, improved solubility of incorporated drug and explored the prospects of manipulation and optimisation of the NPs for intended applications. INTRODUCTION:It has been reported that approximately 40% and even greater number of active pharmaceutical ingredients (APIs) being recognized via combinatory screening programmed are poor water soluble.

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Section: In Vitro Release Profilesupporting

confidence: 88%

Untitled

2016

IJPSR

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“…The hydrophobicity of the polymers may induce unfolding of bFGF molecules; therefore, the bFGF may lose their biological activity after being loaded in and then released from the hydrophobic polymeric systems [8,9] . To promote the advantages and overcome the disadvantages of both the hydrophilic and the hydrophobic polymeric systems, published studies have reported that poly (lactic-co-glycolic acid) (PLGA) and some hydrophilic materials were combined in a composite system [2,8,22,23] , this system worked well for some drugs in vitro, such as insulin [8] , bovine serum albumin [2] , isopropyl myristate [25] , vapreotide [26] , and so on. To create a new biodegradable system for bFGF, a gelatin particle-PLGA micro-sphere composite microsphere was prepared [17][18][19][20] .…”

Section: Introductionmentioning

confidence: 99%

In vitro characteristics of poly(lactic-co-glycolic acid) microspheres incorporating gelatin particles loading basic fibroblast growth factor

Cai

Liu

et al. 2006

Acta Pharmacologica Sinica

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Aim: To construct a sustained drug release system for basic fibroblast growth factor (bFGF). With this special system, bFGF can be used to repair an injured peripheral nerve, injured spinal cord, or as a carrier for other drugs that need to be released over a long time. Methods: Microsphere composite was prepared by encapsulating bFGF into gelatin particles with poly(lactic‐co‐glycolic acid) (PLGA) as its outer‐coating. The encapsulation was conducted by a phase separation method. Results: The average diameter of the gelatin particle‐PLGA microsphere composite was 5–18 um, and bFGF‐loading efficiency was up to 80.5%. The bFGF releasing experiment indicated that this new composite system could release bFGF continuously and protect bFGF from denaturation. Conclusion: A modified approach was successfully employed to develop a biodegradable system for sustained release of the drug of bFGF in vitro.

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“…The surface topography of microspheres prepared from PLA and PLA:PCL is shown in Figures 3 and 4. The microspheres of PLA were smooth and spherical in nature with some very minute pores on their surface, whereas the microspheres prepared with blends of PCL and PLA in the ratio of 1:1 were spherical and highly porous in nature with big pores as clear from to a faster rate of salting out and precipitation of high molecular weight polymer during solvent evaporation compared with those of the lower molecular weight polymer (Elkheshen 1996;Wang et al 1997). …”

Section: Resultsmentioning

confidence: 97%