ABSTRACT
@#As one of the most important biological drugs, protein and peptide drugs have been increasingly used in the prevention, diagnosis and treatment of diseases in recent years. However, most of them need to be injected and lack of long-acting formulations, which brings many troubles to patients suffering from chronic diseases. In this review, we summarized the strategies for engineering long-acting formulations for proteins and peptides via preparation means, including extended-release injection, implant, oral preparations and transdermal drug delivery systems, and analyzed their release mechanisms, research advances, advantages and shortcomings, thereby providing potential approaches for promoting the formulation improvement of these drugs.
ABSTRACT
Objective: To prepare Periplaneta americana extract CII-3-loaded nanoparticles for oral administration, and to investigate the in vitro release profile of CII-3-loaded nanoparticles and the protection of nanoparticles for CII-3 extract in vitro. Methods: The in vitro release behavior of the CII-3-loaded nanoparticles was carried out in the artificial gastric juice, artificial intestinal juice, and pH 7.4 PBS, and the fitting of different models was performed based on the accumulative drug release percentages observed by Folin-reagent method; The amino acid content of CII-3 and CII-3-loaded nanoparticles at different time points in artificial gastric juice was determinated by ninhydrin colorimetry and degradation rates of the two drugs were compared. Results: The mean size of the resulted nanoparticles was about (109.9 ± 0.6) nm and the Zeta potential was (-37.5 ± 3.5) mV; The accumulative release level of CII-3-loaded nanoparticles Qt was (22.63 ± 1.17)% in the artificial gastric juice in the first 2 h, and then, in the artificial intestinal juice, the accumulative release level of CII-3-loaded nanoparticles over a period of 60 h was (72.35 ± 1.90)%, which was in line with Higuchi model release equations, Qt = 8.287 2 t1/2 + 7.758 6. The accumulative release level of CII-3-loaded nanoparticles was (72.67 ± 1.65)% over a period of 10 d, which was in line with Weibull equation, lnln[1/(1-Qt)] = 0.403 7 ln(t-0.411 9)-1.713 3; The CII-3 was completely degraded in 4 h in the artificial gastric juice, while about 70% of CII-3 contained in nanoparticles was degraded. Conclusion: CII-3-loaded nanoparticles have a satisfactory sustained in vitro release effect, and the stability of CII-3 contained in the nanoparticles is improved in the artificial gastric juice.
ABSTRACT
OBJECTIVE: To provide a review of the research progresses of the multivesicular liposomes as a carrier of the protein and peptide drugs. METHODS: To summarize and analyze the researches of the protein/peptide drugs encapsulated in multivesicular liposomes according to the related articles. RESULTS AND CONCLUSION: A major problem in the clinical usage of protein and peptide drugs is frequent injection, for they have poor stability, short half-life time and high clearance. This challenge has been successfully met by the multivesicular liposomes encapsulating the peptide and protein drugs. The new liposome uses depot foam technology to achieve high loading sufficient and encapsulation, and they are very competent carriers of the compounds, especially the water-soluble drugs.
ABSTRACT
Objective To study whether the silica nanoparticles can be used as a biomacromolecular carrier of oral drugs.Methods Studyed the influence of the amount of calcium ions on nano silica nanoparticles morphology,the encapsulation rate of silica nanoparticles on proteins or peptides in the presence of different calcium ions,the situation of proteins or peptides released from silica nanoparticles,enzymolysis of protein packaged by silica, silica nanoparticles labeled peptides with 125 I released in mice.Results Experiments showed that the synthetic silica nanoparticles packaged with peptides could smoothly reach the small intestine through the gastric acid in mice, it had potential to be biomacromolecular carrier of oral drug. Conclusion Proteins or peptides is easy to release in alkaline condition,but release few in acidic condition of pH2 (PH of gastric acid).The silica nanoparticles prepared have the potential to be oral drug carrier.