Study of supramolecular complex of nifedipine with arabinogalactan on Wistar and ISIAH rats

Aim: Physicochemical and pharmacological study of the supramolecular inclusion complexes of the hypotensive drug nifedipine (NF) with the larch polysaccharide arabinogalactan (AG). Materials & methods: The NF:AG complexes were obtained and their physicochemical properties were studied. Their hypotensive action and pharmacokinetic profiles were evaluated in rats with normal and elevated arterial blood pressure. Results: In both rat lines the NF:AG complex decreased the arterial blood pressure at a lower dose than free NF (1.75 mg/kg of NF in complex compared with 3.5 mg/kg of free NF) and has a better pharmacokinetic profile than free NF. Conclusion: The use of the NF:AG complex is an effective way to sufficiently enhance and hasten NF’s hypotensive action.

Clinical efficacy of osteopathic correction in the complex treatment of patients with unoperated open-angle glaucoma

Introduction. Glaucoma is one of the most significant eye diseases. It is often diagnosed, not always amenable to therapy, and can lead to a complete loss of visual functions. In recent years, the method of osteopathic correction has become widespread as one of the effective methods of treatment and rehabilitation of patients with pathologies of various body systems. In the pathogenesis of glaucoma, it is customary to distinguish a dystrophic concept, which considers primary open-angle glaucoma as a result of dystrophic changes in the connective tissue, as well as in the endothelial lining of the trabeculae and Schlemm′s canal, especially destructive changes in mitochondria and the alteration of their functional activity. A vascular concept is also distinguished. According to this concept, the central link in the pathogenesis of glaucoma is circulatory disorder in the ciliary vessels, ocular artery, and major vessels of the head and neck, it can be assumed that osteopathic correction in the treatment of patients with open-angle glaucoma will be pathogenetically substantiated and will have a positive effect on intraocular pressure and trophicity of the optic nerve. The goal of research — to study the influence of in osteopathic correction on the nature of unoperated glaucoma (stage IIA) and to substantiate the possibility of using osteopathic correction in the complex treatment of patients with this pathology.Materials and methods. A prospective controlled randomized study was conducted at 52 city polyclinics, branch 3, Moscow, from January 2018 to January 2019. 40 patients (70 eyes) aged 50 to 75 years with primary open-angle glaucoma IIA stage were examined. At this stage of the disease, patients most often seek medical care and the issue of conservative management is primarily considered. All patients were divided into two groups of 20 people: the main group and the control group. The treatment in the main group included hypotensive drug therapy and osteopathic correction. Patients of the control group received only drug therapy. All patients underwent ophthalmic (visometry, tonometry, perimetry) and osteopathic examination twice: before the treatment and after 3 months.Results. For patients with primary open-angle IIA non-operated glaucoma, regional (most often regions of the head, neck, dura mater) and local (abdominal diaphragm, iliac bones, hip and knee joints) somatic dysfunctions were the most typical. In the main group a statistically significant decrease in the frequency and severity of dysfunctions at all levels was stated. Also, in patients receiving osteopathic correction, a significant decrease in the level of intraocular pressure and perimetric indices was noted. In patients of the control group, no reliable changes in these indicators were obtained.Conclusion. The results obtained indicate that osteopathic correction is clinically effective in the complex treatment of patients with primary open-angle II A glaucoma.

Amphiphilic Acrylic Nanoparticles Containing the Poloxamer Star Bayfit® 10WF15 as Ophthalmic Drug Carriers

Topical application of drops containing ocular drugs is the preferred non-invasive route to treat diseases that affect the anterior segment of the eye. However, the formulation of eye drops is a major challenge for pharmacists since the access of drugs to ocular tissues is restricted by several barriers. Acetazolamide (ACZ) is a carbonic anhydrase inhibitor used orally for the treatment of ocular hypertension in glaucoma. However, large ACZ doses are needed which results in systemic side effects. Recently, we synthesized copolymers based on 2-hydroxyethyl methacrylate (HEMA) and a functionalized three-arm poloxamer star (Bayfit-MA). The new material (HEMA/Bayfit-MA) was engineered to be transformed into nanoparticles without the use of surfactants, which represents a significant step forward in developing new ophthalmic drug delivery platforms. Acetazolamide-loaded nanocarriers (ACZ-NPs) were prepared via dialysis (224 ± 19 nm, −17.2 ± 0.4 mV). The in vitro release rate of ACZ was constant over 24 h (cumulative delivery of ACZ: 83.3 ± 8.4%). Following standard specifications, ACZ-NPs were not cytotoxic in vitro in cornea, conjunctiva, and macrophages. In normotensive rabbits, ACZ-NPs generated a significant intraocular pressure reduction compared to a conventional solution of ACZ (16.4% versus 9.6%) with the same dose of the hypotensive drug (20 µg). In comparison to previously reported studies, this formulation reduced intraocular pressure with a lower dose of ACZ. In summary, HEMA:Bayfit-MA nanoparticles may be a promising system for ocular topical treatments, showing an enhanced ocular bioavailability of ACZ after a single instillation on the ocular surface.

New technologies of hypotensive drug delivery in glaucoma treatment

The paper reports on promising methods of drug delivery in glaucoma treatment: contact lenses, punctum plugs, intraocular implants, subconjunctival and supraciliary injections, ocular rings, hydrogels, nanocarriers.

Cardiotropic action of combined use of celecoxib and amlodipine in rats sicked on adjuvant arthritis coupled with arterial hypertension

Drug therapy of rheumatoid arthritis combined with arterial hypertension is among actual medical objectives. The complexity of pharmacological treatment of comorbid state is due to not only pathological process severity, insufficient efficacy and side effects of disease modifying and symptomatic drugs but also property of nonsteroidal anti-inflammatory drugs (NSAIDs) to aggravate already existed arterial hypertension in patients with rheumatoid arthritis or to increase pressure. Many hypotensive drugs loose or don’t manifest their activity when used in combination with NSAIDs. High risk of cardio toxicity is registered for one of NSAIDs group – coxibs. The cardio safety of combined use of coxibs and hypotensive drugs on the ground of comorbid pathology is studied not enough. These aspects had predefined the aim of this study – to investigate cardiotropic effects of celecoxib when administered in combinations with amlodipine on the ground of experimental rheumatoid arthritis coupled with arterial hypertension. Arterial hypertension was modeled in rats by method of salt load. On the basis of arterial hypertension rheumatoid arthritis was caused by full Freund adjuvant injection. Arterial blood pressure and heart rate registered on sphygmomanometer. It was found that comorbid state is followed by arterial hypertension and tachyarrhythmia. Celecoxib does not facilitate hypertension enhancing but leads to increasing heart rate. Amlodipine manifests specific pharmacological activity as hypotensive drug. The results obtained predefined opportunity of combined use of celecoxib with amlodipine on the ground of rheumatoid arthritis coupled with arterial hypertension.