Determination of Microstructural Impact on the Release of Drug from Hydroxypropyl Cellulose Gel by Validated In Vitro Release Test Method

Author(s):  
Sharda Gurram ◽  
Devanshi S. Shah ◽  
Durgesh K. Jha ◽  
Purnima D. Amin
Author(s):  
Diarmaid J. Murphy ◽  
Deanna Lim ◽  
Ryan Armstrong ◽  
Clare F. McCoy ◽  
Yahya H. Dallal Bashi ◽  
...  

AbstractPreviously reported in vitro release test methods for drug-releasing vaginal rings containing poorly water-soluble drugs have described use of water-alcohol systems or surfactant solutions in efforts to maintain sink conditions. Here, as part of efforts to more closely match in vitro and in vivo release for the 25 mg dapivirine matrix-type silicone elastomer vaginal ring for HIV prevention, we have investigated alternatives to the 1:1 v/v water/isopropanol medium described previously. Specifically, we evaluated dapivirine release from rings into (i) monophasic water/isopropanol mixtures of varying compositions and (ii) biphasic buffer/octanol systems using pH 4.2 and pH 7.0 buffers. The rate and mechanism of dapivirine release were dependent upon the isopropanol concentration in the release medium, in accordance with the observed trend in drug solubility. At 0 and 10% v/v isopropanol concentrations, dapivirine release followed a partition-controlled mechansim. For media containing ≥ 20% v/v isopropanol, in vitro release of dapivirine was significantly increased and obeyed permeation-controlled kinetics. Cumulative release of ~3.5 mg dapivirine over 28 days was obtained using a water isopropanol mixture containing 20% v/v isopropanol, similar to the ~4 mg dapivirine released in vivo. Dapivirine release into the biphasic buffer/octanol system (intended to mimic the fluid/tissue environment in vivo) was constrained by the limited solubility of dapivirine in the buffer component in which the ring resided, such that cumulative dapivirine release was consistently lower than that observed with the 20% v/v isopropanol in water medium. Release into the biphasic system was also pH dependent, in line with dapivirine’s pKa and with potential implications for in vivo release and absorption in women with elevated vaginal pH. Graphical abstract


2020 ◽  
Vol 3 (3) ◽  
pp. 01-07
Author(s):  
Alka Ahuja

Different formulations for the treatment of eye infections are usually administered in the form of conventional ocular drug delivery systems which are topical eye drops or ointments (1). Typically ophthalmic bioavailabilities of only 1–10% are achieved due to the short precorneal residence time of ophthalmic solutions. (2) The preparation and evaluation of gel containing antibiotic azithromycin combined with different polymers like Carbopol, sodium alginate and Hydroxypropyl cellulose (HPC) was done and assessed to find out which polymer could best be used in preparing ophthalmic gels for this antibiotic using factorial design. Since the efficacy of these gels is dependent on factors like viscosity and pH, the polymers in these gels were also examined for different parameters such as pH, in vitro release, permeation and microbiological evaluation.


2008 ◽  
Vol 29 (5) ◽  
pp. 756-762 ◽  
Author(s):  
Jian‐Lei Wang ◽  
Zheng‐Wu Wang ◽  
Feng Liu ◽  
Da‐Yun Zhao

2018 ◽  
Vol 535 (1-2) ◽  
pp. 217-227 ◽  
Author(s):  
Katrin I. Tiffner ◽  
Isadore Kanfer ◽  
Thomas Augustin ◽  
Reingard Raml ◽  
Sam G. Raney ◽  
...  

2011 ◽  
Vol 2011 ◽  
pp. 1-8 ◽  
Author(s):  
Rashmin B. Patel ◽  
Mrunali R. Patel ◽  
Kashyap K. Bhatt ◽  
Bharat G. Patel

A new, simple, and rapid high-performance thin-layer chromatographic method was developed and validated for quantitative determination of Carbamazepine. Carbamazepine was chromatographed on silica gel 60 F254 TLC plate using ethyl acetate-toluene-methanol (5.0 + 4.0 + 1.0 v/v/v) as mobile phase. Carbamazepine was quantified by densitometric analysis at 285 nm. The method was found to give compact spots for the drug (Rf=0.47 ± 0.01). The linear regression analysis data for the calibration plots showed good linear relationship with r2=.9995 in the concentration range 100–600 ng/spot. The method was validated for precision, recovery, repeatability, and robustness as per the International Conference on Harmonization guidelines. The minimum detectable amount was found to be 16.7 ng/spot, whereas the limit of quantitation was found to be 50.44 ng/spot. Statistical analysis of the data showed that the method is precise, accurate, reproducible, and selective for the analysis of Carbamazepine. The method was successfully employed for the estimation of equilibrium solubility, quantification of Carbamazepine as a bulk drug, in commercially available preparation, and in-house developed mucoadhesive microemulsion formulations and solution.


Pharmacia ◽  
2020 ◽  
Vol 67 (2) ◽  
pp. 49-54
Author(s):  
Krassimira Yoncheva ◽  
Nadia Hristova-Avakumova ◽  
Vera Hadjimitova ◽  
Trayko Traykov ◽  
Petar Petrov

The study was focused on the evaluation of two copolymers as micellar carriers for kaempferol delivery. The copolymers comprised identical hydrophilic blocks of poly(2-(dimethylamino)ethyl methacrylate and different hydrophobic blocks of either poly(ε-caprolactone) (PDMAEMA9-b-PCL70-b-PDMAEMA9) or poly(propylene oxide) (PDMAEMA13-b-PPO69-b-PDMAEMA13). The calculation of Flory-Huggins parameters and determination of encapsulation efficiency showed that PDMAEMA-b-PCL-b-PDMAEMA copolymer possessed higher capacity for kaempferol loading. The diameter of the micelles before and after lyophilization was not changed, suggesting that the micelles could be lyophilized and redispersed before administration. The in vitro release of kaempferol from PDMAEMA-b-PPO-b-PDMAEMA micelles was faster than the release from PDMAEMA-b-PCL-b-PDMAEMA micelles, probably due to the higher affinity of kaempferol to this copolymer. Further, the higher affinity resulted in a retention of antioxidant activity of kaempferol in the presence of DPPH and KO2 radicals. Thus, PDMAEMA-PCL-PDMAEMA was considered more appropriate carrier because of the higher encapsulation efficiency and preservation of antioxidant activity of the drug.


2019 ◽  
Vol 15 (4) ◽  
pp. 373-409 ◽  
Author(s):  
Emirhan Nemutlu ◽  
İpek Eroğlu ◽  
Hakan Eroğlu ◽  
Sedef Kır

Background:Nanotech products are gaining more attention depending on their advantages for improving drug solubility, maintenance of drug targeting, and attenuation of drug toxicity. In vitro release test is the critical physical parameter to determine the pharmaceutical quality of the product, to monitor formulation design and batch-to-batch variation.Methods:Spectrophotometric and chromatographic methods are mostly used in quantification studies from in vitro release test of nano-drug delivery systems. These techniques have advantages and disadvantages with respect to each other considering dynamic range, selectivity, automation, compatibility with in vitro release media and cost per sample.Results:It is very important to determine the correct kinetic profile of active pharmaceutical substances. At this point, the analytical method used for in vitro release tests has become a very critical parameter to correctly assess the profiles. In this review, we provided an overview of analytical methods applied to the in vitro release assay of various nanopharmaceuticals.Conclusion:This review presents practical direction on analytical method selection for in vitro release test on nanopharmaceuticals. Moreover, precautions on analytical method selection, optimization and validation were discussed.


Biomolecules ◽  
2021 ◽  
Vol 11 (3) ◽  
pp. 432
Author(s):  
Enkelejda Goci ◽  
Entela Haloci ◽  
Antonio Di Stefano ◽  
Annalisa Chiavaroli ◽  
Paola Angelini ◽  
...  

(1) Background: Capsaicin is the main capsaicinoid of the Capsicum genus and it is responsible for the pungent taste. Medical uses of the fruits of chili peppers date from the ancient time until nowadays. Most of all, they are used topically as analgesic in anti-inflammatory diseases as rheumatism, arthritis and in diabetic neuropathy. Reports state that the Capsicum genus, among other plant genera, is a good source of antimicrobial and antifungal compounds. The aim of this study was the preparation of a pharmaceutical Carbopol-based formulation containing capsaicin and the evaluation of its in vitro release and antimicrobial and antifungal properties. (2) Methods: It was first stabilized with an extraction method from the Capsicum annuum fruits with 98% ethanol and then the identification and determination of Capsaicin in this extract was realized by HPLC. (3) Results and Conclusions: Rheological analyses revealed that the selected formulation exhibited a pseudo-plastic behavior. In vitro release studies of capsaicin from a Carbopol-based formulation reported that approximately 50% of capsaicin was release within 52 h. Additionally, the Carbopol-based formulation significantly increased the antimicrobial effects of capsaicin towards all tested bacteria and fungi strains.


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