Research/Original Articles

Solubility determination and thermodynamic modeling of deferiprone in the binary aqueous mixtures of 2-propanol from 293.15 to 313.15 K

Homa Rezaei , Elaheh Rahimpour, Fleming Martinez , Abolghasem Jouyban

Iranian Journal of Pharmaceutical Sciences, Vol. 19 No. 4 (2023), 24 April 2024, Page 279-292

In the current work, solid-liquid equilibrium measurements and data correlations of deferiprone in 2-propanol + water were carried out. Mathematical models (van’t Hoff, λh, modified Wilson, Jouyban-Acree, and Jouyban-Acree-van’t Hoff) were utilized for correlating the experimental solubility data, and their accuracy was computed by mean relative deviation of the back-calculated data. Furthermore, the apparent thermodynamic parameters of the deferiprone dissolution process were computed by the Gibbs and van’t Hoff equations to analyze the solubility behavior in the investigated mixtures. The results from the analysis and testing of deferiprone solubility data were expected to assist crystallization processes, industrial production, and formulation research.

Ghee based nanostructured lipid carriers (NLCs) with improved wound-healing effects

Mohammad Haji, Marzieh Hosseinzadeh, Yaghoub Jahangiri, Zahra Farajzadeh, Asra Mostashari Sufiani, Yousef Alipour Olyaei, Behnaz Barzegarzadeh Namarvar, Tayyebeh Ghaffari, Nasrin Alipour Olyaei

Iranian Journal of Pharmaceutical Sciences, Vol. 19 No. 4 (2023), 24 April 2024, Page 293-303

Ghee or butter oil is an excellent medium for preparing herbal cosmetics and Ayurvedic medicines formulations. However, water immiscibility restrict its use as a potential carrier system in particular in lipid-based topical formulations. In this work, we prepared ghee-based nanostructured lipid carriers (NLCs) using olive oil as liquid lipid, Tween 60 as surfactant and glycerol as co-surfactant by hot emulsification–ultrasonication method. Then the loaded NLC with a mixture of ethanolic extracts of Achillea millefolium, Horsetail and Plantago major L. was prepared in the same way. NLCs were characterized in terms of size, zeta potential, polydispersity index (PDI) and creaming index. The particle size of NLCs was lower than 100 nm and the zeta potential displayed the negative charge in all formulations. The results of creaming index showed that NLCs were stable for up to 8 weeks under refrigerated conditions. The wound healing effects of the NLCs were evaluated using an excision model in rats. The NLCs displayed significant increased wound contraction and decreased epithelialization period when compare to standard drug phenytoin. This study showed that the ghee-based formulations are much more efficacious in NLC for wound healing promotion in comparison with their macroemulsion form. The formulated system is easy to produce and to apply and could be favourable for topical application in pharmaceutical industries.

Conventional drug delivery methods are not highly efficient due to low bioavailability, poor absorption, and inadequate retention time of some medications. In addition, to achieve the appropriate therapeutic effect, a higher dosage of drugs might be administrated, which may result in undesired side effects. In order to overcome these challenges, utilizing drug delivery systems such as micelles could be beneficial. Micelles are amphiphilic compounds with a hydrophilic shell and a hydrophobic core. Micelles could encapsulate hydrophobic drugs such as Curcumin and tacrolimus, anti-inflammatory and immunosuppressive agents, respectively, and improve their bioavailability. This study synthesized a Methoxy-Polyethyleneglycol-Polycaprolactone biodegradable nano-system by precipitation method for curcumin and tacrolimus encapsulation. Afterward, micelles were characterized for size, morphology, drug loading capacity, and drug release. As a result, the average molecular weight of the copolymer was 36744 g/mol. The nano-system size was analyzed using Dynamic light scattering and Atomic force microscopy tests, resulting in 137.6 nm and 37.9 nm, respectively. In addition, the drug loading efficiency was 42.06%, and after 96 hours, about 0.7mg of Curcumin was released while no Tacrolimus was detected. Since Tacrolimus is retained in the system, we can conclude that this system is not suitable for the simultaneous release of two drugs.

Investigating the effect of Curcumin on Long Noncoding RNAs NUTM2A-AS1 and HCG18 expression changes in Hepatocellular Carcinoma (HCC)

Seyed Ehsan Alavian, Masoud Salehipour, Saeed Zaker Bostanabad, Farzaneh Tafvizi, Mohammad Heiat

Iranian Journal of Pharmaceutical Sciences, Vol. 19 No. 4 (2023), 24 April 2024, Page 314-324

Hepatocellular carcinoma (HCC) is a common tumor in liver tissue. The lack of molecular markers for the diagnosis and evaluation of treatment methods is noticeable despite the progression of HCC diagnostic and treatment methods; therefore, the present study aimed to find molecular markers with key roles in the initiation and progression of HCC and investigate the impact of curcumin on their expression. To this end, bioinformatics studies were conducted to candidate two long noncoding RNAs (lncRNAs) related to HCC, which interacted with the highest number of microRNAs (NUTM2A-AS1 and HCG18), and five microRNAs (hsa-miR-15a-5p, hsa-miR-15b-5p, hsa-miR-16-5p, hsa-miR-195-5p, and hsa-miR-424-5p), which interacted with most lncRNAs among candidate lncRNAs. Afterward, their expression was measured in hepG2 cancer cells and fibroblast cells treated with curcumin compared to the untreated samples. The expression of miRNAs and lncRNAs at half inhibition concentrations (IC50) of curcumin indicated that curcumin significantly increased the expression of miR-195, miR-15a/16, and miR-424 and reduced the expression of miR-15b-5P, NUTM2A-AS1 lncRNA, and HCG18 in comparison with a control group (P≤0.05). Obtained data showed that curcumin increases the expression of anti-cancer genes, miR-195, miR-15a/16, and miR-424, and decreases the activity of cancerous genes, miR-15b-5P, NUTM2A-AS1 lncRNA, and HCG18; therefore, it can be used as an anti-cancer agent in the treatment of HCC.

Copovidone Based Stable Nebivolol Hydrochloride Formulation: Dissolution and Characterization Studies. The study aimed to develop a formulation for the poorly water-soluble drug Nebivolol Hydrochloride. The formulation was carried out in two stages. Stage I attempts to enhance the drug's solubility, while stage II deals with the development of a drug-incorporated tablet formulation. Various strategies with different solid dispersion techniques, like solvent evaporation, melt fusion, and kneading, were used to improve the drug's solubility. Drugs and carriers were mixed with the ratios 1:1, 1:2, 1:3, and 1:4. Apart from the solid dispersion method, the hydrophilic carrier was activated with an acidifier and then mixed with the drug. Preformulation studies were conducted, which included API characterization, solubility measurement over a physiological pH range, and drug-excipients compatibility study. FTIR, DSC, and XRD characterized the developed solid dispersion, which shows the drug exists in the amorphous form in the solid dispersion with no molecular interaction. The dissolution profile revealed a significant improvement in drug solubility with solid dispersion compared to pure drugs. Solid dispersion prepared with Drug, Plasdone, and Tartaric Acid exhibits the most improved solubility and formulated immediate release tablet. Stability studies indicate excellent stability of formulation over six months at accelerated and real-time conditions.

In this study, the purpose of preparing CS/PVA nanofibers loaded GRF microemulsion is to increase the solubility of Low soluble drug griseofulvin by using microemulsion nanocarrier, and nanofiber was used as a technique for a new product. This drug is one of the antifungal drugs, and its uses are for skin diseases. Therefore, a topical route can be a good option. Chitosan /polyvinyl alcohol (CS/PVA) nanofiber containing griseofulvin (GRF) loaded microemulsion was obtained. The microemulsion comprised oleic acid and Transcutol P as the oil phase, Span20 and Labrasol as the surfactant, and Plurol oleique as the cosurfactant. Formulations were prepared with a ME(GRF): polymer ratio (30: 70) and (40: 60) and a polymeric solution containing chitosan (2%) and polyvinyl alcohol (10%) at two weight ratio (20: 80) and (10: 90), respectively. The physicochemical characteristics of the GRF-CS/PVA nanofibers were evaluated. The differential scanning calorimetry (DSC) study showed the amorphous state of the GRF-loaded microemulsions and PVA polymer embedded into the nanofibers. The entrapment efficiency percentage of GRF in the mats was approximately 66.67% - 88.89%. Drug release behavior showed controlled and slow release of drugs that are affected by the type of microemulsion formulation and the ratio of polymers used in nanofibers.

Spectrofluorimetric Determination Method for Pregabalin in Dosage Forms Using 9-Fluorenylmethyl Chloroformate

Effat Souri, Hamed Haramipour, Maliheh Barazandeh Tehrani, Nazanin Shabani Ravari, Roshanak Hariri

Iranian Journal of Pharmaceutical Sciences, Vol. 19 No. 4 (2023), 24 April 2024, Page 350-359

The present study produces a new, accurate, and simple spectrofluorimetric technique for the determination of pregabalin after derivatization with 9-fluorenylmethyl chloroformate in mild basic medium. Pregabalin, containing a primary amine group, reacts with 9-fluorenylmethyl chloroformate, a fluorophore reagent, in borate buffer and produces a fluorescent derivative. The maximum fluorescence intensity of the derivative and reagent was obtained at 315 nm after excitation at 280 nm. The fluorescence intensity of the reagent increases after derivatization with pregabalin, and the difference in the fluorescence intensity is proportional to the concentration of pregabalin. Experimental parameters which affect the derivatization reaction were studied. The best derivatization reaction between pregabalin and 9-fluorenylmethyl chloroformate was obtained after 30 sec. when 40 µg mL-1 of the reagent was used in a borate buffer of pH 9.0. Under optimized conditions, the linearity range (6-150 µg mL-1) of the method with a correlation coefficient of r2 0.9998, accuracy (Error<1.7%), and precision (CV<2.0%) was acceptable. The validated method was utilized for quantifying pregabalin in dosage form without interferences and showed good agreement with a reference method.

The Effect of External Factors on Consumer Buying Behavior in the Cosmetics Market: Evidence from a Developing Country

Razieh Ahmady, Hoda Faraji, Farahnaz Zeinali, Seyed Hesam Sharifnia, Nazila Yousefi

Iranian Journal of Pharmaceutical Sciences, Vol. 19 No. 4 (2023), 24 April 2024, Page 360-367

Consumer decision-making plays a central role in some industries' success and failure, and scholars and practitioners have paid particular attention to the role of consumer behavior styles. This study aims to investigate the effects of product quality, product price, and brand marketing on consumer behavior in the cosmetics industry of a developing country. Data were collected from cosmetics consumers in selected pharmacies in Iran using structured questionnaires. Structural equation modeling was used to test the proposed research hypotheses. The results of this study show that product quality, price, and brand marketing directly influence consumers' behavior toward cosmetic products. Brand marketing was found to have the most significant influence on consumer buying behavior. These findings suggest that it is beneficial for companies to invest in their marketing strategies to gain a competitive advantage.