Zhila Vazifehasl 1,*, Masumeh Alimohammadi 2
1 University of Mohaghegh Ardabili, Ardabil, Iran.
2 Ardabil University of Medical Sciences, Ardabil, Iran.
*Corresponding at University of Mohaghegh Ardabili, Ardabil, Iran, Email: zhila_vazifeh@yahoo.com
Abstract
The main issue for the oil-soluble drugs is their poor aqueous solubility. One proposed technique to deliver oil-soluble drugs is to combine the drug into an inert carrier, such as micro/nanoparticles. The aim of this study is to develop vitamin A palmitate (VAP)-gelatin microspheres to increase its aqueous solubility.
Key words: Vitamin A Palmitate, Microsphere, Solubility
Introduction
Vitamin A is an oil-soluble polyunsaturated hydrocarbon vitamin contains retinol and palmitic acid. It is simply absorbed by the body and is broadly applied in skincare crops. Then, it is a hydrophobic and oxidation sensitive molecule that suffers from rapid degradation in an aqueous environment. Vitamin A palmitate (VAP) is the ester of retinol and palmitic acid. It does not show the oxidation sensitivity [1-3]. Figure 1 shows the VAP chemical structure. An appropriate amount of vitamin A is significant in childhood growth due to its role in ocular health, immune system and nutritional progress. As it cannot be produced in humans, it has to be provided by food or dietary supplements [4,5].
Recently, ultrafine carriers like micro/nanoparticles have confirmed great advantages in terms of increasing the therapeutic efficacy and lessening the side effects by concentrating the therapeutic agents on the wanted places in the body. The use of these systems can also significantly improve the solubility properties of oil-soluble drugs. The properties like dispersibility and stability can be enhanced by encapsulating VAP oil in powder microcapsules by means of an appropriate carrier. This carrier used for encapsulation may also protect against light, oxygen, water, other ingredients [6-10].
Figure 1. VAP chemical structure
Materials and Methods
Materials
Vitamin A palmitate was achieved from AppliChem, Darmstadt, Germany (USP30). The surfactants used were Polyoxymethyl sorbitan monooleate (Mw = 1310 g/mol) (Tween 80) purchased from AppliChem, Darmstadt, Germany. Anhydrous glycerol, 1-propanol and, ethanol were gained from Merck, Darmstadt, Germany, All other chemicals (such as gelatin) were of HPLC grade and were obtained from Merck (Darmstadt, Germany).
Preparation of VAP microspheres
The ratio of surfactant to co-surfactants (anhydrous glycerol, 1-propanol and, ethanol) was fixed at 1:1 on the weight basis. Deionized water was added in different volumes to the mixture of VAP, surfactant and, co-surfactant at room temperature. The sample was stirred for 48 h and 1400 rpm using magnetic stirring. Then, varying the concentration of gelatin were prepared by dissolving in distilled water at 70˚C under gentle stirring for 30 min to improve hydration after cooled to room temperature. Two solutions was added into each other and stirring were continued for 1 h.
Particle characterization
The mean particle size was found by Dynamic Light Scattering (DLS) procedure (Malvern, United Kingdom) at 25 ° C.
Determination of drug content
The accurate weight of 5 mg of microspheres was dissolved and diluted with isopropanol. Using ultraviolet (UV) spectrophotometer (Shimadzu UV-1650, Tokyo, Japan) the absorbance (in triplicate) were measured at 325 nm. Then, the amounts of drug content was calculated via a standard curve.
Solubility
The solubility of microspheres was determined in water by dispersing them in water solution (0.3% w/v). The microspheres were considered soluble once the time of solubilization was not greater than 5 min. The time for total solubilization was also noted [25].
Result and discussion
Particle characterization
The main distinctive property of micro/nanoparticles is their particle size [11]. For the prepared particles, particle size measurement was completed by a dynamic light scattering method. The results showed a mean particle size of 1000 nm (1 micrometer). Figure 2 shows the particle size distribution for the prepared microspheres.
Figure 2. The particle size distribution for the prepared microspheres.
Calculation of drug content
The drug loading is the main factor for a carrier [12]. This amount was calculated to be 48 % for the prepared particles. Results proved that increasing concentration of gelatin increases the loading of VAP in microspheres.
Solubility
The obtained microspheres were tested for the time needed to solubilize in the water. The results showed the time of 2.6 ± 0.25 min for the preparation particles that were less than a time is required for the solubilization of VAP (3.6± 0.90). The results also specified dropping the concentration of gelatin decreases solubility of powder microspheres.
Conclusion
The data found from this study exposed that the used technique (loaded VAP in microspheres) can improve the properties of VAP like solubility.
Conflict of interests
The authors declare that there are no conflicts of interest associated with this work.
References
HOW TO CITE
Vazifehasl, Z., & Alimohammadi, M. (2019). Preparation and study of vitamin A palmitate-gelatin microspheres. Journal of Advanced Chemical and Pharmaceutical Materials (JACPM), 2(1), 97-99. Retrieved from http://advchempharm.ir/journal/index.php/JACPM/article/view/64
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