Improving the dissolution properties of spironolactone using liquisolid technique

Âkbari, Jafar; Saeedi, Majid; Morteza‐Semnani, Katayoun; Sadeghi-Ghadi, Zaynab; Hosseini, Seyed Saeed

doi:10.18869/acadpub.pbr.1.3.59

Cited by 3 publications

(3 citation statements)

References 20 publications

Supporting

Mentioning

Contrasting

Order By: Relevance

“…Figure 4 shows the in vitro SP release from various formulations in phosphate-buffered saline pH 7.4. SP aqueous solubility is 28 µg/mL and all of the release samples contained 1 mg drug [47,51]. To ensure that sink conditions are maintained, a release medium volume of 200 mL was used.…”

Section: Dsc Studiesmentioning

confidence: 99%

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

et al. 2019

View full text Add to dashboard Cite

Spironolactone (SP), an aldosterone antagonist with anti-androgen properties, has shown promising results in the treatment of female acne. However, its systemic side effects limit its clinical benefits. This study aimed to prepare and evaluate LeciPlexes for SP topical delivery. LeciPlexes were prepared by a one-step procedure and characterized using various techniques. Optimum LeciPlex preparation was incorporated into 1% methylcellulose gel and SP permeability was tested ex vivo in Sprague-Dawley rat skin. The maximum drug encapsulation efficiency obtained was 93.6 ± 6.9% and was dependent on the drug/phospholipid and surfactant/phospholipid ratios. A zeta potential of +49.3 ± 3.5 to +57.7 ± 3.3 mV and a size of 108 ± 25.3 to 668.5 ± 120.3 nm were observed for the LeciPlexes. FT-IR and DSC studies confirmed the incorporation of SP into the LeciPlexes through hydrophobic and hydrogen bonding interactions. SP release from the LeciPlex formulations was significantly slower than from the drug suspension. Cumulative SP permeated through rat skin from LeciPlex gel was about 2-fold higher than SP control gel. Cumulative SP deposited in the stratum corneum and other skin layers from the LeciPlex gel was about 1.8- and 2.6-fold higher than SP control gel, respectively. This new SP LeciPlex formulation is a promising carrier for the treatment of female acne.

show abstract

Section: Dsc Studiesmentioning

confidence: 99%

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

et al. 2019

View full text Add to dashboard Cite

show abstract

“…3445, 3420, and 3365 cm −1 another characteristic bands at 3280, 3040 which is corresponding to hydrogen bonded N H. The stretching bands of aromatic C N appeared at 1644, 1618 cm −1 in addition to other characteristic bands for aromatic C N, N O, and C N stretching, these results were in accordance to those mentioned elsewhere 19 concerning the spironolactone. The FTIR spectrum revealed stretching bond C H between 2860 and 3000 cm −1 regions, carbonyl group of lactone (C O) AT 1656 cm −1 , carbonyl stretching bond of thioacetyl at 1690 cm −1 , and vibration of C C at 1617 cm −1 20. In the FTIR of the PM showed most of the characteristic peaks of the two drugs in their proper position confirming the physicochemical compatibility and the absence of interactions between the two drugs (Figure5).…”

mentioning

confidence: 99%

A novel topical combination of minoxidil and spironolactone for androgenetic alopecia: Clinical, histopathological, and physicochemical study

Abdel-Raouf

Aly

Medhat

et al. 2020

Dermatologic Therapy

View full text Add to dashboard Cite

Topical minoxidil 5% are effective in androgenetic alopecia (AGA). Spironolactone acts as an androgen antagonist by competitively blocking androgen receptors. Studying the effect of topical minoxidil 5% gel and spironolactone gel 1% in management of AGA. The study includes 60 patients diagnosed as AGA; (group I): treated with topical minoxidil gel 5%, (group II): with topical spironolactone gel 1% and group (III) treated with combined minoxidil 5% and spironolactone 1% gel. All patients were followed up monthly throughout the treatment period. Scalp biopsy was taken before and after 12 months. In group I, the clinical response was in 90% of patients with variable degrees in improvement, in group II, the clinical response was in 80% of patients, meanwhile, in group III the clinical response was in all patients (100%). Histopathological examination of skin biopsy after treatment revealed significant increase in anagen hair on the other hand, both telogen and vellus hair was significantly decreased meanwhile, the T/V ratio was significantly increased. The results of this work revealed that topical minoxidil gel 5% and topical spironolactone gel 1% were effective in treatment of AGA, while the combination of two agents was better in treatment.

show abstract

“…The results obtained justifies that the cinnarizine in the solid liquid formulations has lost its crystalline structure and the drug is present in its molecularly dispersed state. Thus, we can conclude that cinnarizine has been completely solubilized in Propylene Glycol [24].…”

Section: Ftir Studiesmentioning

confidence: 70%

Cinnarizine Liquid Solid Compacts: Preparation Evaluation

Sisinthy

Selladurai

2019

Int J App Pharm

View full text Add to dashboard Cite

Objective: The objective of this research was to formulate cinnarizine tablets using the liquid-solid compact technique to enhance its solubility and dissolution rate.Methods: Cinnarizine liquid-solid compacts were formulated using propylene glycol as the non-volatile solvent, Neusilin US2 as the carrier material, Aerosil 200 as the coating material and croscarmellose sodium as the disintegrant. The interaction between drug and excipients were characterized by Fourier-transform infrared spectroscopy (FTIR) and differential scanning calorimetry (DSC) studies. Different batches of liquid, solid compacts were prepared by using varying carrier-coating excipient ratio and different concentration of liquid medication. Flow parameters such as bulk density, tapped density, Carr’s Index, Hausner’s Ratio as well as an angle of repose were used to test the flowability of the powder blend. The liquid-solid compacts were produced by direct compression method and were evaluated for tests such as weight variation, drug content, hardness, thickness, friability, wetting time, disintegration time as well as the in vitro dissolution studies.Results: The results of the preformulation studies of liquisolid compacts showed acceptable flow properties. The results of FTIR and DSC studies showed that there is no drug-excipient interactions. The different R values and concentrations were found to have a marked effect on the dissolution profile. Formulations with higher carrier: coating ratio (R-value) and lower drug concentrations displayed a better dissolution profile. The percentage of drug release of F3 with an R-value of 20 and a drug concentration of 10% was found to be 88.11% when compared to the conventional marketed tablet which released only 44.07% at the end of 2 h.Conclusion: From this research, it is inferred that liquid-solid technique is a promising and effective approach that can be used to enhance the dissolution rate of cinnarizine.

show abstract

Improving the dissolution properties of spironolactone using liquisolid technique

Cited by 3 publications

References 20 publications

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

Spironolactone-Loaded LeciPlexes as Potential Topical Delivery Systems for Female Acne: In Vitro Appraisal and Ex Vivo Skin Permeability Studies

A novel topical combination of minoxidil and spironolactone for androgenetic alopecia: Clinical, histopathological, and physicochemical study

Cinnarizine Liquid Solid Compacts: Preparation Evaluation

Contact Info

Product

Resources

About