Displaying publications 1 - 20 of 160 in total

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  1. Loke YH, Chew YL, Janakiraman AK, Lee SK, Uddin ABMH, Goh CF, et al.
    Drug Dev Ind Pharm, 2024 Jan;50(1):36-44.
    PMID: 38149637 DOI: 10.1080/03639045.2023.2294095
    INTRODUCTION: Orally disintegrating tablets (ODTs) are designed to dissolve in the oral cavity within 3 min, providing a convenient option for patients as they can be taken without water. Direct compression is the most common method used for ODTs formulations. However, the availability of single composite excipients with desirable characteristics such as good compressibility, fast disintegration, and a good mouthfeel suitable for direct compression is limited.

    OBJECTIVE: This research was proposed to develop a co-processed excipient composed of xylitol, mannitol, and microcrystalline cellulose for the formulation of ODTs.

    METHODS: A total of 11 formulations of co-processed excipients with different ratios of ingredients were prepared, which were then compressed into ODTs, and their characteristics were thoroughly examined. The primary focus was on evaluating the disintegration time and hardness of the tablets, as these factors are important in ensuring the ODTs meet the desired criteria. The model drug, Mirtazapine was then incorporated into the chosen optimized formulation.

    RESULTS: The results showed that the formulation comprised of 10% xylitol, 10% mannitol and 80% microcrystalline cellulose demonstrated the fastest disintegration time (1.77 ± 0.119 min) and sufficient hardness (3.521 ± 0.143 kg) compared to the other formulations. Furthermore, the drug was uniformly distributed within the tablets and fully released within 15 min.

    CONCLUSION: Therefore, the developed co-processed excipients show great potential in enhancing the functionalities of ODTs, offering a promising solution to improve the overall performance and usability of ODTs in various therapeutic applications.

    Matched MeSH terms: Drug Compounding/methods
  2. Nurkolis F, Taslim NA, Hardinsyah H
    Clin Nutr ESPEN, 2023 Aug;56:81-82.
    PMID: 37344087 DOI: 10.1016/j.clnesp.2023.05.008
    Potential studies and evidence regarding nutrient nanoencapsulation combined with emulsion-based delivery systems are relatively limited. Therefore, for the importance issue of health vision, with this critical opinion to the editor is scientifically important to invite worldwide researchers to raise their concern for clinical research and the development of plant-based lutein nanoencapsulation in staple foods in alleviating nutritional problems for the eyes, which has not been reported before. This is in line with the WHO World Report which aimed to overcome the challenge regarding vision and galvanizing action, one of which is through innovation and research. With the hypothesis that, through this opinion will increase the awareness of scientists to improve clinical studies on the stability and bioaccessibility of lutein for health vision concern. As our hypothesis and objectives, we hope that this critical short opinion to the editor will assist efforts to reduce the burden of eye conditions and vision loss to achieve the Sustainable Development Goals (SDGs), particularly SDG 3.8 on universal health coverage through lutein-plant based nanoencapsulation clinical studies by worldwide researchers. Finally, it is very important and needed an effort to improve clinical studies focus on the stability and bioaccessibility of lutein for health vision via lutein-plant based nanoencapsulation approaches. Moreover, the benefit of lutein supplementation for the health vision might be limited by its bioaccessibility and bioavailability. Future studies and approaches should employ strategies that could overcome the foregoing limitations, of which is through nanoencapsulation approach. Something new has been synthesized in this work, "Because, every human eye, is the eye of the world".
    Matched MeSH terms: Drug Compounding*
  3. Abd Kadir E, Uchegbu IF, Schätzlein AG
    Int J Pharm, 2023 Jun 10;640:123036.
    PMID: 37169106 DOI: 10.1016/j.ijpharm.2023.123036
    Disulfiram (DS) is an anti-alcoholism drug capable of acting against important and hard-to-treat cancers. The drug's relative instability and variable absorption/distribution have led to its variable pharmacokinetics and suboptimal exposure. Hence, it was hypothesised that a nano-enabled form of DS might be able to overcome such limitations. Encapsulation of the labile DS was achieved with quaternary ammonium palmitoyl glycol chitosan (GCPQ) to form a high-capacity, soybean oil-based DS-GCPQ nanoemulsion. DS-GCPQ showed capability of oil-loading up to 50% v/v for a stable entrapment of high drug content. With increasing oil content (10 to 50% v/v), the mean particle size and polydispersity index were also increased (166 to 351 nm and 0.14 to 0.22, respectively) for a given amount of GCPQ. Formulations showed a highly positive particle surface charge (50.9 ± 1.3 mV), contributing to the colloidal stability of the individual particles. DS-GCPQ showed marked cytotoxicity against pancreatic cancer cell lines with enhanced activity in the presence of copper. An intravenous pharmacokinetic study of DS-GCPQ in vivo showed improved plasma drug stability with a DS half-life of 17 min. Prolonged survival was seen in tumour-bearing animals treated with DS-GCPQ supplemented with copper. In conclusion, DS-GCPQ nanoemulsion has the potential to be developed further for cancer therapeutic purposes.
    Matched MeSH terms: Drug Compounding
  4. Veronica N, Heng PWS, Liew CV
    Expert Opin Drug Deliv, 2023 Jan;20(1):115-130.
    PMID: 36503355 DOI: 10.1080/17425247.2023.2158183
    INTRODUCTION: As a nature-derived polymer with swelling and gelling properties, alginate has found wide biopharma-relevant applications. However, there is comparatively limited attention on alginate in tablet formulations. Therefore, this review aimed to provide an overview of the applications of alginate in solid dosage form formulations.

    AREAS COVERED: This review outlines the role of alginate for oral sustained release formulations. For better insights into its application in drug delivery, the mechanisms of drug release from alginate matrices are discussed alongside the alginate inherent properties and drug properties. Specifically, the influence of alginate properties and formulation components on the resultant alginate gel and subsequent drug release is reviewed. Modifications of the alginate to improve its properties in modulating drug release are also discussed.

    EXPERT OPINION: Alginate-based matrix tablets is useful for sustaining drug release. As a nature-derived polymer, batch consistency and stability raise some concerns about employing alginate in formulations. Furthermore, the alginate gel properties can be affected by formulation components, pH of the dissolution environment and the tablet matrix micro-environment pH. Conscientious efforts are pivotal to addressing these formulation challenges to increase the utilization of alginate in oral solid dosage forms.

    Matched MeSH terms: Drug Compounding
  5. Kumar P, Chaudhary B, Jain V, Baboota S, Shivanandy P, Alharbi KS, et al.
    Curr Drug Deliv, 2023;20(9):1262-1274.
    PMID: 36380413 DOI: 10.2174/1567201820666221114113637
    Molecular pharmaceutics play a critical role in the drug delivery system, representing the direct interconnection of drug bioavailability with its molecular form. There is a diversity in the molecular structures by which it affects its properties, such as amorphous form, crystalline form, partialamorphous molecular dispersion, and disordered state. The active pharmaceutical ingredient (API) and the excipients utilized in the formulation process contain various divergent modes used in the formulation process. They include better formulations of any type to obtain good quality pharmaceutical products. This review reveals how the molecular states affect the API and are important in maintaining the quality of dosage forms. Furthermore, the physio-chemical properties of the components and various pharmaceutical approaches employed in the formulation of dosage forms are studied from the point of view of molecular pharmaceutics.
    Matched MeSH terms: Drug Compounding
  6. Corrie L, Gulati M, Kaur J, Awasthi A, Vishwas S, Ramanunny AK, et al.
    Curr Drug Res Rev, 2023;15(3):272-285.
    PMID: 36683365 DOI: 10.2174/2589977515666230120140543
    BACKGROUND: Curcumin (CRM) is known to possess various therapeutic properties, such as anti-inflammatory and antidiabetic properties, and is, therefore, considered to be an effective therapeutic.

    OBJECTIVE: A sensitive method for the estimation of CRM in plasma, as well as fecal matter-based solid self-nano emulsifying drug delivery system (S-SNEDDS), has been reported for the first time.

    METHODS: A bioanalytical method was optimized using Box-Behnken Design having 13 runs and 3 responses. The optimized method was developed using methanol and water (70:30 v/v) with a flow rate of 1 mL/min. Quercetin was used as an internal standard. A specificity test was also performed for the developed CRM solid self-nano emulsifying drug delivery system.

    RESULTS: The retention time of CRM was found to be 14.18 minutes. The developed method was validated and found to be linear in the range of 50-250 ng/mL with an R2 of 0.999. Accuracy studies indicated that CRM had a percentage recovery of less than 105% and more than 95%, respectively. Precision studies were carried out for inter, intraday, and inter-analyst precision, and the %RSD was found to be less than 2%. The limit of detection (LOD) and limit of quantification (LOQ) were found to be 3.37 ng/mL and 10.23 ng/mL, respectively. Stability studies for shortterm, long term and freeze-thaw cycles showed a %RSD of less than 2%, indicating the stability of CRM in the plasma matrix. Moreover, the blank fecal microbiota extract slurry did not show any peak at the retention time of CRM in a CRM-loaded solid nanoemulsifying drug delivery system containing fecal microbiota extract indicating its specificity.

    CONCLUSION: Hence, the developed method can have clinical implications as it helps estimate CRM in blood samples and also provides a simple and sensitive method for the estimation of plant-based flavonoids along with fecal microbiota extract formulations.

    Matched MeSH terms: Drug Compounding
  7. Pandian K, Kalayarasi J, Gopinath SCB
    Biotechnol Appl Biochem, 2022 Dec;69(6):2766-2779.
    PMID: 35287249 DOI: 10.1002/bab.2321
    This study presents a novel sulfur-doped graphitic carbon nitride (S@g-C3 N4 ) with a wider potential range as electrocatalyst for electrochemical sensor application. The S@g-C3 N4 nanosheets were successfully prepared with a ball milling method by mixing appropriate molar concentration required precursors. The as-synthesized heteroatom-doped graphitic carbon nitride is characterized by spectroscopic techniques including PL, DRS-UV, FT-IR, and Brunauer-Emmett-Teller equation. The morphological features were studied by FE-SEM and HR-TEM analysis. Chit-S@g-C3 N4 -modified glassy carbon electrode (GCE) was employed for the electrochemical detection of omeprazole (OMZ) use in drug formulations. We have noted an oxidation peak current response at a potential of +0.8 V versus Ag/AgCl in PBS medium (0.1 M, pH 7.0). Differential pulse voltammetry amperometry experimental method can be used to measure the concentration of OMZ for quantitative studies in known samples. Under the optimized experimental condition, the calibration plot was constructed by plotting the peak currents versus OMZ in the linear ranges from 6.0 × 10-7 to 26 × 10-5  M. The linear regression equation is estimated to be Ip (μA) = 0.9518 (C/μM) + 0.3340 with a good correlation coefficient of 0.9996. The lower determination limit was found to be 20 nM and the current sensitivity was calculated (31.722 μA μM-1  cm-2 ). The developed sensor was utilized successfully to determine the OMZ concentration in drug formulations and biological fluids. These results revealed that the Chit-S@g-C3 N4 -modified GCE showed excellent electroanalytical performance for the detection of OMZ at a low LOD, wider linear range, high sensitivity, good reproducibility, long-term storage stability, and selectivity with an acceptable relative standard deviation value.
    Matched MeSH terms: Drug Compounding
  8. Azmi NHS, Ming LC, Uddin ABMH, Sarker ZI, Bin LK
    Int J Pharm Compd, 2022 1 27;26(1):80-87.
    PMID: 35081048
    Oral drug delivery has been recognized as the most desirable drug administration method among other drug delivery routes due to its ease of administration, long shelf life, and low cost. Orally disintegrating tablets disintegrate within seconds in the mouth without the need of water for swallowing. This unique feature of orally disintegrating tablets is favorable to special populations such as geriatric and pediatric patients. Formulation optimization is significant to obtain the optimal combination of tablet constituents, as the tablet composition is influential on dosage-form characteristics. The objective of this study was to investigate the effect of different types of fillers and percentage on the physical properties of orally disintegrating tablets by using amlodipine as the model drug. Blank orally disintegrating tablets containing different fillers, namely, Sorbolac 400, Granulac 200, and CombiLac with different percentages, were prepared using the wet granulation method and were evaluated based on weight variation, hardness, thickness, friability, and disintegration time. Formulation 5 that consists of 25% Granulac 200 showed the optimal result among all formulations with the fastest disintegration time (96.17 s Å} 18.40) and sufficient tablet hardness (4.59 kg Å} 0.70). Hence, formulation 5 was selected as the optimal formulation and incorporated with amlodipine. From this study, it can be concluded that excipients have an essential role in determining the physical properties of orally disintegrating tablets.
    Matched MeSH terms: Drug Compounding
  9. Samrot AV, Saigeetha S, Mun CY, Abirami S, Purohit K, Cypriyana PJJ, et al.
    Sci Rep, 2021 12 31;11(1):24511.
    PMID: 34972829 DOI: 10.1038/s41598-021-03328-2
    Latex, a milky substance found in a variety of plants which is a natural source of biologically active compounds. In this study, Latex was collected from raw Carica papaya and was characterized using UV-Vis, FTIR and GC-MS analyses. Super Paramagnetic Iron Oxide Nanoparticles (SPIONs) were synthesized, coated with C. papaya latex (PL-Sp) and characterized using UV-Vis, FT-IR, SEM-EDX, XRD, VSM and Zeta potential analyses. SPIONs and latex coated SPIONs (PL-Sp) were used in batch adsorption study for effective removal of Methylene blue (MB) dye, where (PL-Sp) removed MB dye effectively. Further the PL-Sp was used to produce a nanoconjugate loaded with curcumin and it was characterized using UV-Vis spectrophotometer, FT-IR, SEM-EDX, XRD, VSM and Zeta potential. It showed a sustained drug release pattern and also found to have good antibacterial and anticancer activity.
    Matched MeSH terms: Drug Compounding
  10. Khursheed R, Singh SK, Wadhwa S, Gulati M, Kapoor B, Jain SK, et al.
    Int J Biol Macromol, 2021 Oct 31;189:744-757.
    PMID: 34464640 DOI: 10.1016/j.ijbiomac.2021.08.170
    The role of mushroom polysaccharides and probiotics as pharmaceutical excipients for development of nanocarriers has never been explored. In the present study an attempt has been made to explore Ganoderma lucidum extract powder (GLEP) containing polysaccharides and probiotics to convert liquid self nanoemulsifying drug delivery system (SNEDDS) into solid free flowing powder. Two lipophilic drugs, curcumin and quercetin were used in this study due to their dissolution rate limited oral bioavailability and poor permeability. These were loaded into liquid SNEDDS by dissolving them into isotropic mixture of Labrafill M1944CS, Capmul MCM, Tween-80 and Transcutol P. The liquid SNEDDS were solidified using probiotics and mushroom polysaccharides as carriers and Aerosil-200 as coating agent. The solidification was carried out using spray drying process. The process and formulation variables for spray drying process of liquid SNEDDS were optimized using Box Behnken Design to attain required powder properties. The release of both drugs from the optimized spray dried (SD) formulation was found to be more than 90%, whereas, it was less than 20% for unprocessed drugs. The results of DSC, PXRD and SEM, showed that the developed L-SNEDDS preconcentrate was successfully loaded onto the porous surface of probiotics, mushroom polysaccharides and Aerosil-200.
    Matched MeSH terms: Drug Compounding
  11. Farhana A, Koh AE, Tong JB, Alsrhani A, Kumar Subbiah S, Mok PL
    Molecules, 2021 Sep 06;26(17).
    PMID: 34500845 DOI: 10.3390/molecules26175414
    Molecular crosstalk between the cellular epigenome and genome converge as a synergistic driver of oncogenic transformations. Besides other pathways, epigenetic regulatory circuits exert their effect towards cancer progression through the induction of DNA repair deficiencies. We explored this mechanism using a camptothecin encapsulated in β-cyclodextrin-EDTA-Fe3O4 nanoparticles (CPT-CEF)-treated HT29 cells model. We previously demonstrated that CPT-CEF treatment of HT29 cells effectively induces apoptosis and cell cycle arrest, stalling cancer progression. A comparative transcriptome analysis of CPT-CEF-treated versus untreated HT29 cells indicated that genes controlling mismatch repair, base excision repair, and homologues recombination were downregulated in these cancer cells. Our study demonstrated that treatment with CPT-CEF alleviated this repression. We observed that CPT-CEF exerts its effect by possibly affecting the DNA repair mechanism through epigenetic modulation involving genes of HMGB1, APEX1, and POLE3. Hence, we propose that CPT-CEF could be a DNA repair modulator that harnesses the cell's epigenomic plasticity to amend DNA repair deficiencies in cancer cells.
    Matched MeSH terms: Drug Compounding
  12. Azad AK, Doolaanea AA, Al-Mahmood SMA, Kennedy JF, Chatterjee B, Bera H
    Int J Biol Macromol, 2021 Aug 31;185:861-875.
    PMID: 34237363 DOI: 10.1016/j.ijbiomac.2021.07.019
    Peppermint oil (PO) is the most prominent oil using in pharmaceutical formulations with its significant therapeutic value. In this sense, this oil is attracting considerable attention from the scientific community due to its traditional therapeutic claim, biological and pharmacological potential in recent research. An organic solvent-free and environment-friendly electrohydrodynamic assisted (EHDA) technique was employed to prepared PO-loaded alginate microbeads. The current study deals with the development, optimization, in vitro characterization, in vivo gastrointestinal tract drug distribution and ex-vivo mucoadhesive properties, antioxidant, and anti-inflammatory effects of PO-loaded alginate microbeads. The optimization results indicated the voltage and flow rate have a significant influence on microbeads size and sphericity factor and encapsulation efficiency. All these optimized microbeads showed a better drug release profile in simulated intestinal fluid (pH 6.8) at 2 h. However, a minor release was found in acidic media (pH 1.2) at 2 h. The optimized formulation showed excellent mucoadhesive properties in ex-vivo and good swelling characterization in intestine media. The microbeads were found to be well distributed in various parts of the intestine in in vivo study. PO-loaded alginate microbeads similarly showed potential antioxidant effects with drug release. The formulation exhibited possible improvement of irritable bowel syndrome (IBS) in MO-induced rats. It significantly suppressed proinflammatory cytokines, i.e., interleukin- IL-1β, and upregulated anti-inflammatory cytokine expression, i.e., IL-10. It would be a promising approach for targeted drug release after oral administration and could be considered an anti-inflammatory therapeutic strategy for treating IBS.
    Matched MeSH terms: Drug Compounding
  13. Liew KB, Peh KK
    Arch Pharm Res, 2021 Aug;44(8):1-10.
    PMID: 25579848 DOI: 10.1007/s12272-014-0542-y
    Orally disintegrating tablet (ODT) is a user friendly and convenient dosage form. The study aimed to investigate the effect of polymers and wheat starch on the tablet properties of lyophilized ODT, with dapoxetine as model drug. Three polymers (hydroxypropylmethyl cellulose, carbopol 934P and Eudragit® EPO) and wheat starch were used as matrix forming materials in preparation of lyophilized ODT. The polymeric dispersion was casted into a mould and kept in a freezer at -20 °C for 4 h before freeze dried for 12 h. It was found that increasing in HPMC and Carbopol 934P concentrations produced tablets with higher hardness and longer disintegration time. In contrast, Eudragit® EPO was unable to form tablet with sufficient hardness at various concentrations. Moreover, HPMC seems to have a stronger effect on tablet hardness compared to Carbopol 934P at the same concentration level. ODT of less friable was obtained. Wheat starch acted as binder which strengthen the hardness of ODTs and prolonged the disintegration time. ODT comprising of HPMC and wheat starch at ratio of 2:1 was found to be optimum based upon the tablet properties. The optimum formulation was palatable and 80 % of the drug was released within 30 min in the dissolution study.
    Matched MeSH terms: Drug Compounding/methods
  14. Khursheed R, Singh SK, Gulati M, Wadhwa S, Kapoor B, Pandey NK, et al.
    Int J Biol Macromol, 2021 Jul 31;183:1630-1639.
    PMID: 34015408 DOI: 10.1016/j.ijbiomac.2021.05.064
    Ganoderma lucidium extract powder (GLEP) contains various polysaccharides which are well known for their antioxidant and anti-inflammatory actions. Probiotics (PB) are well-established for providing a plethora of health benefits. Hence, use of mushroom polysaccharides and probiotics as carriers to solidify liquisolid formulation is anticipated to function as functional excipients i.e. as adsorbent that may provide therapeutic benefits. Quercetin (QUR) has been used as model lipophilic drug in this study. QUR loaded liquisolid compacts (LSCs) were formulated using Tween 80 as solvent. These were further solidified using a combination of PB and GLEP as carriers. Aerosil-200 (A-200) was used as coating agent. The formulation exhibited very good flow characteristics. Dissolution rate of raw QUR was found to be less than 10% in 60 min while in case of QUR loaded LSCs, more than 90% drug release was observed within 5 min. Absence of crystalline peaks of QUR in the DSC and PXRD reports of LSCs and their porous appearance in SEM micrographs indicate that QUR was successfully incorporated in the LSCs. The developed formulation was found to be stable on storage under accelerated stability conditions.
    Matched MeSH terms: Drug Compounding
  15. Kaur J, Mishra V, Singh SK, Gulati M, Kapoor B, Chellappan DK, et al.
    J Control Release, 2021 06 10;334:64-95.
    PMID: 33887283 DOI: 10.1016/j.jconrel.2021.04.014
    Amphiphilic block copolymers are widely utilized in the design of formulations owing to their unique physicochemical properties, flexible structures and functional chemistry. Amphiphilic polymeric micelles (APMs) formed from such copolymers have gained attention of the drug delivery scientists in past few decades for enhancing the bioavailability of lipophilic drugs, molecular targeting, sustained release, stimuli-responsive properties, enhanced therapeutic efficacy and reducing drug associated toxicity. Their properties including ease of surface modification, high surface area, small size, and enhanced permeation as well as retention (EPR) effect are mainly responsible for their utilization in the diagnosis and therapy of various diseases. However, some of the challenges associated with their use are premature drug release, low drug loading capacity, scale-up issues and their poor stability that need to be addressed for their wider clinical utility and commercialization. This review describes comprehensively their physicochemical properties, various methods of preparation, limitations followed by approaches employed for the development of optimized APMs, the impact of each preparation technique on the physicochemical properties of the resulting APMs as well as various biomedical applications of APMs. Based on the current scenario of their use in treatment and diagnosis of diseases, the directions in which future studies need to be carried out to explore their full potential are also discussed.
    Matched MeSH terms: Drug Compounding
  16. Eghbali Babadi F, Yunus R, Masoudi Soltani S, Shotipruk A
    ACS Omega, 2021 May 04;6(17):11144-11154.
    PMID: 34056270 DOI: 10.1021/acsomega.0c04353
    In this study, a mineral-based coated urea was fabricated in a rotary pan coater using a mixture of gypsum/sulfur/zeolite (G25S25Z50) as an effective and low-cost coating material. The effects of different coating compositions on the dissolution rate of urea and the crushing strength and morphology of the coated urea were investigated. A 25:25:50 (wt %) mixture of gypsum/sulfur/zeolite (G25S25Z50) increased the coating effectiveness to 34.1% with the highest crushing strength (31.06 N). The effectiveness of coated urea was further improved to 46.6% with the addition of a microcrystalline wax (3%) as a sealant. Furthermore, the release mechanisms of various urea fertilizers were determined by fitting the release profiles with six mathematical models, namely, the zeroth-order, first-order, second-order, Higuchi, Ritger & Peppas, and Kopcha models. The results showed that the release mechanism of the uncoated urea and all other coated urea followed the Ritger & Peppas model, suggesting the diffusional release from nonswellable delivery systems. In addition, due to the increased mass-transfer resistance, the kinetic constant was decreased from 0.2233 for uncoated urea to 0.1338 for G25S25Z50-coated urea and was further decreased to 0.0985 when 3% Witcovar 146 sealant was applied.
    Matched MeSH terms: Drug Compounding
  17. Kuang TK, Kang YB, Segarra I, Kanwal U, Ahsan M, Bukhari NI
    Turk J Pharm Sci, 2021 04 20;18(2):167-175.
    PMID: 33902255 DOI: 10.4274/tjps.galenos.2020.48902
    Objectives: This study was conducted to assess the effect of microwave heating on the preparation of paracetamol cross-linked gelatin matrices by using the design of experiment (DoE) approach and explore the influence of the duration of microwave irradiation, the concentrations of crosslinker, and the amount of sodium bicarbonate (salt) on paracetamol release. These parameters were also compared with those of the matrices prepared via conventional heating.

    Materials and Methods: Twenty gel matrices were prepared with different durations of microwave irradiation, amounts of maize, and concentrations of sodium bicarbonate as suggested by Design Expert (DX®). The percentage drug release, the coefficient of variance (CV) in release, and the mean dissolution time (MDT) were the properties explored in the designed experimentation.

    Results: Target responses were dependent on microwave irradiation time, cross-linker amount, and salt concentration. Classical and microwave heating did not demonstrate statistically significant difference in modifying the percentage of drug released from the matrices. However, the CVs of microwave-assisted formulations were lower than those of the gel matrices prepared via classical heating. Thus, microwave heating produced lesser variations in drug release. The optimized gel matrices demonstrated that the observed percentage of drug release, CV, and MDT were within the prediction interval generated by DX®. The release mechanism of the matrix formulations followed the Peppas-Korsmeyer anomalous transport model.

    Conclusion: The DoE-supported microwave-assisted approach could be applied to optimize the critical factors of drug release with less variation.

    Matched MeSH terms: Drug Compounding
  18. Chaudhary S, Nair AB, Shah J, Gorain B, Jacob S, Shah H, et al.
    AAPS PharmSciTech, 2021 Apr 09;22(3):127.
    PMID: 33835317 DOI: 10.1208/s12249-021-01995-y
    Being a candidate of BCS class II, dolutegravir (DTG), a recently approved antiretroviral drug, possesses solubility issues. The current research was aimed to improve the solubility of the DTG and thereby enhance its efficacy using the solid dispersion technique. In due course, the miscibility study of the drug was performed with different polymers, where Poloxamer 407 (P407) was found suitable to move forward. The solid dispersion of DTG and P407 was formulated using solvent evaporation technique with a 1:1 proportion of drug and polymer, where the solid-state characterization was performed using differential scanning calorimetry, Fourier transform infrared spectroscopy and X-ray diffraction. No physicochemical interaction was found between the DTG and P407 in the fabricated solid dispersion; however, crystalline state of the drug was changed to amorphous as evident from the X-ray diffractogram. A rapid release of DTG was observed from the solid dispersion (>95%), which is highly significant (p<0.05) as compared to pure drug (11.40%), physical mixture (20.07%) and marketed preparation of DTG (35.30%). The drug release from the formulated solid dispersion followed Weibull model kinetics. Finally, the rapid drug release from the solid dispersion formulation revealed increased Cmax (14.56 μg/mL) when compared to the physical mixture (4.12 μg/mL) and pure drug (3.45 μg/mL). This was further reflected by improved bioavailability of DTG (AUC: 105.99±10.07 μg/h/mL) in the experimental Wistar rats when compared to the AUC of animals administered with physical mixture (54.45±6.58 μg/h/mL) and pure drug (49.27±6.16 μg/h/mL). Therefore, it could be concluded that the dissolution profile and simultaneously the bioavailability of DTG could be enhanced by means of the solid dispersion platform using the hydrophilic polymer, P407, which could be projected towards improved efficacy of the drug in HIV/AIDS.
    Matched MeSH terms: Drug Compounding
  19. Shao M, Li S, Tan CP, Kraithong S, Gao Q, Fu X, et al.
    Int J Biol Macromol, 2021 Mar 15;173:118-127.
    PMID: 33444656 DOI: 10.1016/j.ijbiomac.2021.01.043
    In this study, caffeine (CA) was encapsulated into food-grade starch matrices, including swelled starch (SS), porous starch (PS), and V-type starch (VS). The bitterness of the microcapsules and suppression mechanisms were investigated using an electronic tongue, molecular dynamics (MD) simulation and the in vitro release kinetics of CA. All the CA-loaded microcapsules showed a lower bitterness intensity than the control. The MD results proved that the weak interactions between starch and CA resulted in a moderate CA release rate for SS-CA microcapsules. The PS-CA microcapsule presented the longest CA release, up to 40 min, whereas the VS-CA microcapsule completely released CA in 9 min. The CA release rate was found to be related to the microcapsule structure and rehydration properties. A low CA bitterness intensity could be attributed to a delay in the CA release rate and resistance to erosion of the microcapsules. The results of this work are valuable for improving starch-based microcapsules (oral-targeted drug-delivery systems) by suppressing the bitterness of alkaloid compounds.
    Matched MeSH terms: Drug Compounding/methods*
  20. Abou Assi R, Abdulbaqi IM, Siok Yee C
    Pharmaceuticals (Basel), 2021 Mar 04;14(3).
    PMID: 33806527 DOI: 10.3390/ph14030215
    Current research indicates that the next silent epidemic will be linked to chronic liver diseases, specifically non-alcoholic fatty liver disease (NAFLD), which was renamed as metabolic-associated fatty liver disease (MAFLD) in 2020. Globally, MAFLD mortality is on the rise. The etiology of MAFLD is multifactorial and still incompletely understood, but includes the accumulation of intrahepatic lipids, alterations in energy metabolism, insulin resistance, and inflammatory processes. The available MAFLD treatment, therefore, relies on improving the patient's lifestyle and multidisciplinary pharmacotherapeutic options, whereas the option of surgery is useless without managing the comorbidities of the MAFLD. Nanotechnology is an emerging approach addressing MAFLD, where nanoformulations are suggested to improve the safety and physicochemical properties of conventional drugs/herbal medicines, physical, chemical, and physiological stability, and liver-targeting properties. A wide variety of liver nanosystems were constructed and delivered to the liver, only those that addressed the MAFLD were discussed in this review in terms of the nanocarrier classes, particle size, shape, zeta potential and offered dissolution rate(s), the suitable preparation method(s), excipients (with synergistic effects), and the suitable drug/compound for loading. The advantages and challenges of each nanocarrier and the focus on potential promising perspectives in the production of MAFLD nanomedicine were also highlighted.
    Matched MeSH terms: Drug Compounding
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