Development of technology for obtaining nifedipine nanoparticles to improve its solubility

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Abstract

Introduction. Nifedipine, a typical representative of 1,4-dihydropyridine, is widely used in the treatment of various diseases due to its vasodilatory and antihypertensive effects. Low water solubility is a common problem for drugs such as nifedipine, limiting their bioavailability and effectiveness. This leads to a decrease in the therapeutic effect and the need to increase the dosage, which, in turn, can increase the risk of side effects. Nanotechnology offers a promising approach to overcome this barrier, allowing the creation of dosage forms with improved pharmacokinetic properties.

Aim of the study. Developing a method for increasing the solubility of nifedipine by obtaining nanoparticles using a high-energy ball mill.

Material and methods. The following were used in the work: nifedipine (Tamico, Syria), methanol (Biosolve Chimie, France), potassium dihydrogen phosphate, sodium heptanesulfonate and orthophosphoric acid (85%) (Isolab, Germany), purified water and Tween 20 (Merck, Germany). Nifedipine was ground using a high-energy ball mill (Retsch PM 400). During the research, the dissolution profile of nifedipine and nifedipine nanoparticles was studied by examining their saturated solution using HPLC. To characterize the sizes of the ground samples, they were examined using scanning electron microscopy (SEM).

Results. The use of a high-energy ball mill (Retsch PM 400) allowed us to obtain nifedipine nanoparticles with significantly improved solubility characteristics. It was found that the solubility of nifedipine nanoparticles was 9.05%, which is 38 times higher than that of the original substance (0.24%).

Conclusions. The findings of this study highlight the transformative potential of high-energy ball milling in enhancing the solubility of nifedipine, a crucial component in pharmaceutical formulations. By employing this innovative approach, we successfully produced nifedipine nanoparticles with demonstrably improved solubility compared to the conventional powder form. This achievement opens a new frontier in the development of nifedipine-based dosage forms with enhanced bioavailability. The increased solubility of nifedipine nanoparticles signifies a promising avenue for optimizing drug delivery and potentially improving therapeutic efficacy.

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About the authors

N. J. Dahma

Belgorod State National Research University

Author for correspondence.
Email: narmeendahma@gmail.com
ORCID iD: 0009-0000-6421-6052

Post-graduate Student, Institute of Pharmacy, Chemistry and Biology

Russian Federation, st. Pobeda, 85, Belgorod, 308015

E. T. Zhiljakova

Belgorod State National Research University

Email: narmeendahma@gmail.com
ORCID iD: 0000-0002-8685-1601
SPIN-code: 9169-7991

Professor, Dr.Sc. (Pharm.), Head of the Department of Pharmaceutical Technology

Russian Federation, st. Pobeda, 85, Belgorod, 308015

M. J. Dahma

Pirogov Russian National Research Medical University of the Ministry of Health of the Russian Federation

Email: narmeendahma@gmail.com
ORCID iD: 0009-0003-0838-6657

Post-graduate Student, Institute of Dentistry

Russian Federation, st. Ostrovityanova, 1, Moscow, 117513

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Supplementary files

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2. Fig. 1. SEM micrographs of unmilled nifedipine

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3. Fig. 2. SEM micrographs of nifedipine nanoparticles

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4. Fig. 3. Dissilution profile of nifedipine

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5. Fig. 4. Dissilution profile of nifedipine nanoparticals

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6. Fig. 5. Dissilution profile of nifedipine and nifedipine nanoparticles

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