Minocycline hydrochloride nano sustained-release gel as well as preparation method and application thereof

Abstract

The invention discloses minocycline hydrochloride nano sustained-release gel as well as a preparation method and application thereof, and belongs to the technical field of medicines. The problem of low encapsulation efficiency of small-molecule hydrophilic medicines is solved by introducing a form of a novel complex formed by chelating minocycline hydrochloride, metal ions and a compound with a plurality of sulfate, sulfonate or phosphate functional groups. Prepared minocycline hydrochloride multiple emulsion nanoparticles are smooth, round, high in encapsulation efficiency and strong in drug loading capacity. A prepared minocycline hydrochloride multiple emulsion nanoparticle is dispersed in a temperature-sensitive gel matrix to construct a double-layer delivery system which has certain biological adhesion, is good in periodontal retention and is convenient for administration. According to the minocycline hydrochloride nano sustained-release gel as well as the preparation method and application thereof, while the positioning advantage of the gel is exerted, burst release of a medicine can be remarkably reduced, the medicine administration period can be prolonged, possibility is created for further periodontal pocket local medicine administration treatment of periodontitis, the nanoparticles can penetrate through alveolar bone trabecula and bottom connective tissue, distribution of the medicine at a focus position is enhanced, and the antibacterial effect of the medicine is remarkably improved.

Description

technical field [0001] The invention belongs to the technical field of medicines, and in particular relates to a minocycline hydrochloride nano sustained-release gel and a preparation method and application thereof. Background technique [0002] Periodontitis is a common chronic oral disease, clinically manifested as inflammation and bleeding of the gums, formation of periodontal pockets, loss of attachment, and destruction of alveolar bone resorption, which eventually leads to tooth loosening and loss, which is the main cause of tooth loss in adults. Among many pathogenic factors, bacterial infection is the main factor for inducing and maintaining inflammation. At the same time, due to the complex structure of periodontal pockets, it is difficult for mechanical scaling to effectively remove deep microorganisms and lead to recurrence of lesions. Therefore, basic mechanical scaling is supplemented with Local antibiotic treatment has become a trend in the treatment of periodon...

AI Technical Summary

Problems solved by technology

So far, the periodontal local sustained-release preparations that have been on the market are mainly the following: 1. Fiber type, the trade name is However, due to its non-biodegradable characteristics, it has been discontinued; 2. Film type, It is an absorbable film product, but its size and shape are poorly variable, easy to fall off after administration, and patient compliance is poor

3. Microsphere type, FDA approved minocycline microspheres in 2001 For the treatment of chronic periodontitis, because the powdery microspheres are difficult to stay in the periodontal disease for a long time, so its application is limited; 4. Gel / ointment type, doxycycline gel and minocycline hydrochloride ointment All of them have been approved by the FDA for the treatment of periodontitis, but the disadvantage is that the slow-release effect is poor, and there is often an initial burst-release effect

However, compared with lipophilic drugs, the encapsulation efficiency of hydrophilic small molecule drugs is usually lower, and it is difficult to achieve an effective concentration at the lesion site, because the water-soluble drug molecules may be distributed to the external water successively before the formulation is solidified. and was removed

The water solubility of the drug can be changed by introducing a drug, metal ion and a compound with multiple sulfate, phosphate or sulfonate functional groups to chelate to form a new complex, so as to solve the problem of small molecule hydrophilic drugs The problem of low encapsulation rate

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