Composition of analgesic bioadhesive healing microspheres

Abstract

A new composition of analgesic bioadhesive healing microspheres in which each microsphere comprises at least:a.—a layer of a polyanion, where the polyanion may be an alginate.b.—a core coated with a polyanion consisting of a triblock copolymer non-ionic surfactant; polexamer 188 or a mixture of them; and a volatile halogenated by-product anaesthetic ether agent of methyl-isopropyl-ether in contact with the internal part of the polyanion layer, which may be sevoflurane.c.—a coating of a polycation in contact with the external part of the polyanion layer, which may be chitosan.

Description

THE SUBJECT OF THE INVENTION[0001]This invention refers to a new pharmaceutical composition, cost-effective in production, for algic treatment and to enhance healing of cutaneous lesions or of the oral mucosa where the healing process deteriorates and with loss of substance, epithelium and / or conjunctiva, comprising microspheres composed of a triblock copolymer non-ionic surfactant core or a mixture, such as poloxamer 188, and a volatile halogenated ether agent such as fluoromethyl 2.2.2-trifluoro-1-(trifluoromethyl)ethyl ether; a layer of polyanion such as sodium alginate; and a coating of polycation such as chitosan.PRIOR ART[0002]2.5 million cases of chronic ulcer (of venous and arterial etiology) in the lower limbs are registered annually in the United States. Their presence is associated with pain, restriction on work activities and leisure, reduced mobility, sleep disorders, reduced psychological well-being and social isolation. They also represent a major financial burden for...

AI Technical Summary

Benefits of technology

The invention is a new pharmaceutical composition that can be used to treat chronic ulcers, particularly those in the lower limbs, with a focus on reducing pain and promoting healing. The composition is made up of microspheres composed of a non-ionic surfactant core, a volatile halogenated ether agent, and a coating of polycation. The composition has been found to be effective in treating pain associated with vascular ulcers and has been shown to have a lower impact on the healing process compared to other treatments. The invention addresses the need for an effective treatment for chronic vascular ulcers with tendency to torpid evolution.

Problems solved by technology

Their presence is associated with pain, restriction on work activities and leisure, reduced mobility, sleep disorders, reduced psychological well-being and social isolation.

They also represent a major financial burden for healthcare systems.

There is at present a lack of scientific evidence about the effectiveness of the various topical treatments for the pain associated with vascular ulcers.

Their analgesic effectiveness is limited, in other words they have an analgesic ceiling, their analgesia not being dose-dependent, so that increased dose may prolong the effect but does not produce more analgesia and raises the incidence of side effects.

They are effective in the treatment of slight-moderate pain and in some cases may control intense pain with an inflammatory component, but the use of anti-inflammatory non steroid drugs and opiates in the elderly population with a high associated comorbidity is accompanied by a high rate of adverse effects.

Any intervention which relieves pain but significantly slows healing is likely to prove clinically unacceptable, unless it is clear that the ulcer is very unlikely to heal.

It can thus be asserted that there is not at present an effective treatment for chronic vascular ulcers with tendency to torpid evolution.

In addition to their hypnotic effect on the nervous system, their analgesic effect has also been demonstrated at the central level, but research intended to find a peripheral-level analgesic effect has failed, so that they are at present considered to lack such effect.

2011 saw the publication of the first case (M. Gerónimo-Pardo et al) of a patient with a very painful vascular ulcer, where the therapy was based on different combinations of analgesics (such as paracetamol, metamizole, tramadole, morphine, fentanyl, buprenorphine, pregabalin and gabapentin, as well as applications of eutectic lidocaine / prylocaine and infusion of epidural ropivacaine), and was completely unsatisfactory.