OBJECTIVETo prepare and evaluate the injectable temperature responsive in situ gel for sustained release of Glabrous Sarcandra Herb extract in vitro.

METHODThe novel temperature responsive poloxamer 407 was used as the carrier material of Glabrous Sarcandra Herb extract sustained release injection. The release of Glabrous Sarcandra Herb extract from poloxamer 407 based in situ gel in the phosphate buffer (pH 7. 6) was studied at 37 degrees C under agitation. HPLC method was used for the determination of Glabrous Sarcandra Herb extract.

RESULTThe best prescription was composed of by 16% P-407, 6% P-188, 0.2% HPMC, 0.5% benzil alcohol and 4% (g mL(-1)) Glabrous Sarcandra Herb extract. The optimal gelation temperature was around 33 degrees C. The data of release in vitro were analyzed according to the theoretical model of Korsmeyer-Peppas.

CONCLUSIONThe preparation method of the injectable thermosensitive in situ gel of Glabrous Sarcandra Herb extract is appropriate. The release in vitro can reach the expecting request.

PURPOSE: To evaluate the compatibility of poloxamer hydrogel as a material for the injectable intraocular lens in in vivo and in vitro model. METHODS: We determined the appropriate concentration of poloxamer hydrogel for injection through the examination of transparency and gelling temperature of this material and assess the technique of refilling the lens capsule and the postoperative findings. RESULTS: Poloxamer hydrogel showed excellent transparency compared with balanced salt solution(BSS) in air vinyl and 20% was identified as an appropriate concentration for direct lens refilling material. In vivo study, we injected poloxamer into the capsular bag after performing endocapsular phacoemulsification through the small anterior capsulotomy site. At 3 months follow up, we confirmed the excellent transparency and biocompatibility of poloxamer hydrogel. CONCLUSIONS: Poloxamer hydrogel was identified as an appropriate material for direct lens refilling material.
Follow-Up Studies ; Hydrogel* ; Lenses, Intraocular* ; Phacoemulsification ; Poloxamer ; Polymers*

Objective: To observe the effect of poloxamer 188 (P188) on megakaryocyte cultivation and induction from cord blood mononuclear cells in order to obtain more megakaryocyte progenitor cells (MPC). Methods: The cord blood mononuclear cells were isolated and inoculated in cell culture bag or cell culture flask respectively. The WIGGENS shaker and cell culture bags were used to mimick WAVE Bioreactor for three-dimensional (3D) cell culture, and the P188 was added to induction medium, The cells were detected for morphology, surface marker, viability, and number on day 14. Results: In the two-dimensional (2D) culture, CD41(+), CD41(+)/CD61(+), CD61(+) megakaryocytic numbers increased significantly after adding P188 (all P<0.01). And in the 3D culture of adding P188, the cell volume became larger and the nuclear shape was irregular, the cytoplasm appeared magenta granules, and the megakaryocyte cells became more mature. By 3D culture, the expression of CD41/CD61 was (36.30±1.27)% vs (23.95±1.34)%, hence the differentiation for MPC was significantly higher than that in the 2D group (P<0.01). Furthermore, adding P188 in 3D culture resulted in highest differentiation efficiency for MPC [(59.45±1.20)%]. There were no significantly differences in terms of cell viability and cell number among 3D culture containing P188, 2D and 3D culture groups (all P>0.05). Conclusion: 3D culture was beneficial for the differentiation of MPC, but the cell viability was lower than 2D group; However, the satisfied cell growth and better induction efficiency were obtained by adding of P188, which might provide a new method of megakaryocytes production for clinical application.
Bioreactors ; Cell Differentiation ; Cells, Cultured ; Fetal Blood ; Megakaryocytes ; Poloxamer

PURPOSE: This study was designed to induce irreVersible gel formation of poloxamer, the thermosensitive polymer hydrogel, by using photoinitiator and UV irradiation, and to verify the biocompatibility and usability of poloxamer as an injectable intraocular lens material through long-term observation in vivo. METHODS: Endocapsular phacoemulsification of lens was performed in rabbits and 25% poloxamer mixed with various concentrations of photoinitiator was injected into the capsular bag through a small capsulorhexis site. Then, the whole eye was irradiated with UV light for 5 minutes. The irreversibility and transparency of the post-operative poloxamer and the effects on the conjunctiva, cornea, iris, vitreous humor and retina were observed. RESULTS: As the results of this experiment using poloxamer 25% and photoinitiator 0.01%, the poloxamer remained transparent in the lens capsule for more than six months after the operation. No inflammatory response or toxicity was observed on the conjunctiva, cornea, iris, vitreous humor or retina. CONCLUSIONS: This study demonstrated the possibility of poloxamer as a new material for the injectable intraocular lens. Further study, however, is necessary.
Capsulorhexis ; Conjunctiva ; Cornea ; Hydrogel ; Iris ; Lenses, Intraocular* ; Phacoemulsification ; Poloxamer ; Polymers ; Rabbits* ; Retina ; Ultraviolet Rays ; Vitreous Body

PURPOSE: The occurrence of post-surgical adhesion is still a major cause of postoperative morbidity due to the lack of satisfactory treatment or prophylaxis. Several adhesion barriers have been developed in the form of solutions or membrane in an attempt to solve these problems. However both types of tissue barriers have some limitations in their practical applications. In order to overcome these problems, a temperature-sensitive Poloxamer/Alginate/CaCl2 mixture was prepared as an adhesion barrier. With this material, toxicity, inflammation and the adhesion prevention effect was evaluated in an animal model. METHODS: The sol-gel transition behavior was measured using a viscometer. An in vitro gel stability test and an in vivo degradation test was performed. The anti-adhesion effect was evaluated using a cecal-abdominal wall abrasion model. The denuded cecum was coated with Poloxamer/ Alginate/CaCl2 mixture, GUARDIX-SL (positive control group) or neither (negative control group) and apposed to the abdominal wall (each n=14). One week after surgery, the level of adhesion was graded from zero to three using a whole-number system. RESULTS: The LCST of the poloxamer/sodium alginate mixture was 25 degrees C. The gel stability of Poloxamer was improved by adding mild cross-linked sodium Alginate/CaCl2 mixture. The adhesion grade and area were significantly lower in the experimental group than in the control. CONCLUSION: The anti-adhesive effect of the Poloxamer/Alginate/CaCl2 mixture was comparable to the previously- developed solution type barrier and all the materials had degraded within 21 days. From these results, Poloxamer/ Alginate/CaCl2 mixture is a good candidate for use as a coatable or injectable tissue adhesion barrier.
Abdominal Wall ; Animals ; Cecum ; Inflammation ; Membranes ; Models, Animal* ; Poloxamer ; Rats* ; Sodium ; Tissue Adhesions

Pluronic modified polyamidoamine (PAMAM) conjugate (PF127-PAMAM) was prepared and the inhibiting effect of MDR against MCF-7/ADR was investigated with doxorubicin (DOX) as model drug. 1H NMR and FTIR spectra showed that the conjugate was synthesized successfully. Element analysis accurately measured that 27.63% amino of per PAMAM was modified by pluronic (PAMAM : PF127, 1 : 35.37 mole ratio). PF127-PAMAM showed an increased size and a reduced zeta potential compared to PAMAM. PF127-PAMAM had lower hemolytic toxicity and cytotoxicity due to the reduced zeta potential and the protection of PF127. Each PF127-PAMAM molecular could load 19.58 DOX molecules, and the complex exhibited sustained and pH-sensitive release behavior. PF127-PAMAM/DOX exhibited weaker cytotoxicity than free DOX in MCF-7 cells; while the complex showed much stronger reverse effect of drug resistance in MCF-7/ADR cells, and resistance reversion index (RRI) was as high as 33.15.
Dendrimers ; pharmacology ; Doxorubicin ; pharmacology ; Humans ; MCF-7 Cells ; drug effects ; Poloxamer ; pharmacology

With low molecular weight chitosan and poloxamer 188 as the joint carriers, ginsenoside Rg3 solid dispersions were prepared by using the solvent evaporation method for an in vitro dissolution test. Subsequently, differential scanning calorimetry (DSC), scanning electron microscopy (SEM) and X-ray diffraction (X-RD) were adopted for a phase analysis. The results showed that the 60 min in vitro cumulative dissolution rate of ginsenoside Rg3 solid dispersions prepared with low molecular weight chitosan and poloxamer 188 at the ratio of 2:1 exceeded 90%, and the drug was dispersed in carriers in an amorphous state. Therefore, ginsenoside Rg3 solid dispersions prepared with low molecular weight chitosan and poloxamer 188 could help significantly improve the drug dissolution, with a practical application value.
Chitosan ; chemistry ; Drug Compounding ; methods ; Ginsenosides ; chemistry ; Molecular Weight ; Poloxamer ; chemistry ; Solvents ; chemistry

OBJECTIVETo observe the biodegradation and absorption of poloxamer 407 in vivo, and the effect of poloxamer 407 on the middle ear and inner ear after regional perfusion in guinea pigs.

METHODSThe right ears of 10 guinea pigs as experimental group were perfused with 20% poloxamer 407 in situ gel 100 microl in round window niche, with the left ears as control group with normal saline. Another two animals without treatment were in negative control group. Auditory function was investigated before and 3, 7, 14, 28, 49 days after perfusion, and the histology of bulles after auditory brainstem response (ABR) each examination were examined by means of serial section after paraffin imbedding.

RESULTSThe poloxamer gel was almost biodegraded and discharged 49 days after perfusion, only few gel remained in the middle ear cavity under light microscope. The ABR threshold to filtered clicks was elevated after perfusion with poloxamer 407, and was recovered to normal at 49 days after perfusion. The morphology of the mucosa of middle ear cavity, round window membrane, Corti's and vestibular organs were not significantly damaged after poloxamer 407 perfusion.

CONCLUSIONSPoloxamer 407 can be biodagraded in vivo or discharged via eustachian tube, and causes no inflammation on the middle ear cavity. There are temporary changes on auditory function of inner ear after topical perfusion with poloxamer 407 in round window can cause, but no irreversible damage on function and morphology of cochlear and vestibular organs.

The objectives of this study are to prepare resveratrol loaded mixed micelles composed of poloxamer 403 and poloxamer 407, and optimize the formulation in order to achieve higher drug solubility and sustained drug release. Firstly, a thin-film hydration method was utilized to prepare the micelles. By using drug-loading, encapsulation yield and particle size of the micelles as criteria, influence of three variables, namely poloxamer 407 mass fraction, amount of water and feeding of resveratrol, on the quality of the micelles was optimized with a central composite design method. Steady fluorescence measurement was carried out to evaluate the critical micelle concentration of the carriers. Micelle stability upon dilution with simulated gastric fluid and simulated intestinal fluid was investigated. The in vitro release of resveratrol from the mixed micelles was monitored by dialysis method. It was observed that the particle size of the optimized micelle formulation was 24 nm, with drug-loading 11.78%, and encapsulation yield 82.51%. The mixed micelles increased the solubility of resveratrol for about 197 times. Moreover, the mixed micelles had a low critical micelle concentration of 0.05 mg · mL(-1) in water and no apparent changes in particle size and drug content were observed upon micelles dilution, indicating improved kinetic stability. Resveratrol was released from the micelles in a controlled manner for over 20 h, and the release process can be well described by Higuchi equation. Therefore, resveratrol-loaded poloxamer 403/407 mixed micelles could improve the solubility of resveratrol significantly and sustained drug release behavior can be achieved.
Drug Carriers ; chemistry ; Fluorescence ; Kinetics ; Micelles ; Particle Size ; Poloxamer ; chemistry ; Solubility ; Stilbenes ; chemistry ; Water

Drug Carriers ; Drug Combinations ; Drugs, Chinese Herbal ; administration & dosage ; Poloxamer ; Polyethylene Glycols ; Solubility ; Technology, Pharmaceutical ; methods