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Enhanced Solubility and Bioavailability of Dolutegravir by Solid Dispersion Method: In Vitro and In Vivo Evaluation-a Potential Approach for HIV Therapy

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
Vesicular Systems Containing Curcumin and Their Applications in Respiratory Disorders - A Mini Review

Chellappan DK, Hansbro PM, Dua K, Hsu A, Gupta G, Ng ZY, et al.

Pharm Nanotechnol, 2017;5(4):250-254.
PMID: 28786351 DOI: 10.2174/2211738505666170808094635

BACKGROUND: Vesicular systems like nanotechnology and liposomes are gaining tremendous attention lately in the field of respiratory diseases. These formulations enhance bioavailability of the drug candidate, which could be achieved through a novel drug delivery mechanism. Moreover, the therapeutic potential achieved through these systems is highly controllable over long durations of time providing better efficacy and patient compliance.
OBJECTIVE: The objective of this paper is to review the recent literature on vesicular drug delivery systems containing curcumin.
METHODS: We have collated and summarized various recent attempts made to develop different controlled release drug delivery systems containing curcumin which would be of great interest for herbal, formulation and biological scientists. There are several vesicular nanotechnological techniques involving curcumin which have been studied recently, targeting pulmonary diseases.
RESULTS: Different vesicular systems containing curcumin are being studied for their therapeutic potential in different respiratory diseases. There has been a renewed interest in formulations containing curcumin recently, primarily owing to the broad spectrum therapeutic potential of this miracle substance. Various types of formulations, containing curcumin, targeting different bodily systems have recently emerged and, nevertheless, the search for newer frontiers with this drug goes on.
CONCLUSION: This mini review, in this direction, tries to highlight the key research interventions employing vesicular systems of drug delivery with curcumin.

Matched MeSH terms: Drug Compounding/methods
Comparative biodistribution and safety profiling of olmesartan medoxomil oil-in-water oral nanoemulsion

Gorain B, Choudhury H, Tekade RK, Karan S, Jaisankar P, Pal TK

Regul Toxicol Pharmacol, 2016 Dec;82:20-31.
PMID: 27815174 DOI: 10.1016/j.yrtph.2016.10.020

Poor aqueous solubility and unfavourable de-esterification of olmesartan medoxomil (a selective angiotensin II receptor blocker), results in low oral bioavailability of less than 26%. Improvement of oral bioavailability with prolonged pharmacodynamics activity of olmesartan in Wistar rats had been approached by nanoemulsification strategy in our previous article [Colloid Surface B, 115, 2014: 286]. In continuation to that work, we herewith report the biodistribution behaviour and 28-day repeated dose sub-chronic toxicity of olmesartan medoxomil nanoemulsion in Wistar rats following oral administration. The levels of olmesartan in collected biological samples were estimated using our validated LC-MS/MS technique. Our biodistribution study showed significantly higher brain concentrations of olmesartan (0.290 ± 0.089 μg/mL, 0.333 ± 0.071 μg/mL and 0.217 ± 0.062 μg/mL at 0.5, 2.0 and 8.0 h post dosing, respectively) when administered orally as nanoemulsion formulation as compared to the aqueous suspension. In addition, the olmesartan nanoemulsion was found to be safe and non-toxic, as it neither produced any lethality nor remarkable haematological, biochemical and structural adverse effects as observed during the 28-days sub-chronic toxicity studies in experimental Wistar rats. It is herewith envisaged that the developed nanoemulsion formulation approach for the delivery of olmesartan medoxomil via oral route can further be explored in memory dysfunction and brain ischemia, for better brain penetration and improved clinical application in stroke patients.

Matched MeSH terms: Drug Compounding
Fulltext A Time-Domain NMR Study of the State of Water in Wet Granules with Different Fillers and Its Contribution to the Wet Granulation Process and to the Characteristics of Granules

Ito T, Okada K, Leong KH, Hirai D, Hayashi Y, Kumada S, et al.

Chem Pharm Bull (Tokyo), 2019;67(3):271-276.
PMID: 30828004 DOI: 10.1248/cpb.c18-00888

The different states of water incorporated in wet granules were studied by a low-field benchtop 1H-NMR time-domain NMR (TD-NMR) instrument. Wet granules consisting different fillers [cornstarch (CS), microcrystalline cellulose (MCC), and D-mannitol (MAN)] with different water contents were prepared using a high-speed granulator, and then their spin-spin relaxation time (T2) was measured using the NMR relaxation technique. The experimental T2 relaxation curves were analyzed by the two-component curve fitting, and then the individual T2 relaxation behaviors of solid and water in wet granules were identified. According to the observed T2 values, it was confirmed that the molecular mobility of water in CS and MCC granules was more restricted than that in the MAN granule. The state of water appeared to be associated with the drying efficiency and moisture absorption capacity of wet granules. Thus, it was confirmed that the state of water significantly affected the wet granulation process and the characteristics of the resultant granules. In the final phase of this study, the effects of binders on the molecular mobility of water in granulation fluids and wet granules were examined. The state of water in granulation fluids was substantially changed by changing the binders. The difference was still detected in wet granules prepared by addition of these fluids to the fillers. In conclusion, TD-NMR can offer valuable knowledge on wet granulation from the viewpoint of molecular mobility of water.

Matched MeSH terms: Drug Compounding/methods*
Fulltext Physiochemical properties of Kenaf seed oil microcapsules before and after freeze drying and its storage stability

Hue, W.L., Nyam, K.L.

International Food Research Journal, 2018;25(4):1502-1509.
MyJurnal

Kenaf seed oil contains high amount of monounsaturated fatty acid (MUFA) and polyunsaturated fatty acid (PUFA), and bioactive compounds, such as tocopherol and phytosterol. In order to prevent bioactive compounds from oxidation, kenaf seed oil (KSO) was encapsulated by coextrusion technology. KSO and microencapsulated kenaf seed oil (MKSO) were then subjected to accelerated storage to investigate the effect of microencapsulation on the storage stability of kenaf seed oil. The changes of fatty acids profiles and bioactive compounds in oils were evaluated. Result showed that there was significant decreased (p

Matched MeSH terms: Drug Compounding
Effects of Accelerated Storage on the Quality of Kenaf Seed Oil in Chitosan-Coated High Methoxyl Pectin-Alginate Microcapsules

Leong MH, Tan CP, Nyam KL

J Food Sci, 2016 Oct;81(10):C2367-C2372.
PMID: 27635525 DOI: 10.1111/1750-3841.13442

The objective of this research was to study the oxidative stability and antioxidant properties of microencapsulated kenaf (Hibiscus cannabinus L.) seed oil (MKSO) produced by co-extrusion technology upon accelerated storage. The combination of sodium alginate, high methoxyl pectin, and chitosan were used as shell materials. The oxidative stability of the kenaf seed oil was determined by iodine value, peroxide value, p-Anisidine value, total oxidation (TOTOX), thiobarbituric acid reactive substances assay, and free fatty acid content. Total phenolic content, 2,2'-azino-bis(3-ethylbenzothiazoline-6-sulphonic acid) cation radical-scavenging assay and 2,2-diphenyl-1-picrylhydrazyl radical scavenging assay were used to examine the antioxidant properties of oils. Oxidative stability tests showed that bulk kenaf seed oil (BKSO) was oxidized significantly higher (P < 0.05) than MKSO. The total increment of TOTOX value of BKSO was 165.93% significantly higher (P < 0.05) than MKSO. Co-extrusion technology has shown to be able to protect kenaf seed oil against lipid oxidation and delay the degradation of natural antioxidants that present in oil during storage.

Matched MeSH terms: Drug Compounding*
Effect of Gum Arabic, β-Cyclodextrin, and Sodium Caseinate as Encapsulating Agent on the Oxidative Stability and Bioactive Compounds of Spray-Dried Kenaf Seed Oil

Chew SC, Tan CP, Nyam KL

J Food Sci, 2018 Sep;83(9):2288-2294.
PMID: 30074623 DOI: 10.1111/1750-3841.14291

Kenaf seed oil is prone to undergo oxidation due to its high content of unsaturated fatty acids, thus microencapsulation stands as an alternative to protect kenaf seed oil from the adverse environment. This study primarily aimed to evaluate the oxidative stability of microencapsulated refined kenaf seed oil (MRKSO) by the use of gum arabic, β-cyclodextrin, and sodium caseinate as the wall materials by spray drying. Bulk refined kenaf seed oil (BRKSO) and MRKSO were kept at 65 °C for 24 days to evaluate its oxidative stability, changes of tocopherol and tocotrienol contents, phytosterol content, and fatty acid profile. The results showed that the peroxide value, p-Anisidine value, and total oxidation value of BRKSO were significantly higher than the MRKSO at day 24. The total tocopherol and tocotrienol contents were reduced 66.1% and 56.8% in BRKSO and MRKSO, respectively, upon the storage. There was a reduction of 71.7% and 23.5% of phytosterol content in BRKSO and MRKSO, respectively, upon the storage. The degradation rate of polyunsaturated fatty acids in BRKSO was higher than that of MRKSO. This study showed that the current microencapsulation technique is a feasible way to retard the oxidation of kenaf seed oil.
PRACTICAL APPLICATION: There is increasing research on the functional properties of crude kenaf seed oil, but the crude kenaf seed oil is not edible. This study offered in developing of microencapsulated refined kenaf seed oil by spray drying, which is suitable for food application. The microencapsulation of refined kenaf seed oil with healthier wall materials is beneficial in developing a diversity of functional food products and supplements.

Matched MeSH terms: Drug Compounding/methods*
Fulltext Preparation and Evaluation Pumpkin Seed Oil-based Vitamin E Cream Formulations for Topical Application

Ong TS, Chu CC, Tan CP, Nyam KL

J Oleo Sci, 2020;69(4):297-306.
PMID: 32249259 DOI: 10.5650/jos.ess19250

Plant seed oil is often incorporated into the cream emulsions to provide multifunctional effects on the skin. In the current study, pumpkin seed oil (PSO) was used to develop a stable oil-in-water emulsion. The study aimed to optimise PSO cream formulation and determine the synergistic effect of the PSO with vitamin E oil added. The physical properties, antioxidant activities and storage stability of the formulations were analysed. Besides, the synergistic effect of the best formulation was analysed based on α-tocopherol content using ultra-high performance liquid chromatography (UHPLC). The storage stability test was assessed upon storing at 25 ± 2°C and 40 ± 2°C for 12 weeks. The best formulation (20% PSO, vitamin E oil and beeswax) selected showed physically and microbiologically stable. The incorporation of vitamin E oil into the formulation produced with PSO was found to be compatible, as it showed a synergistic effect in the amount of α-tocopherol content (combination index (CI) = 0.98). Thus, PSO had shown its potency to be incorporated into the topical products with a promising potential in delivering additional properties that can nourish the skin.

Matched MeSH terms: Drug Compounding*
Sustained-release alginate-chitosan pellets prepared by melt pelletization technique

Wong TW, Nurulaini H

Drug Dev Ind Pharm, 2012 Dec;38(12):1417-27.
PMID: 22309449 DOI: 10.3109/03639045.2011.653364

Alginate-chitosan pellets prepared by extrusion-spheronization technique exhibited fast drug dissolution.

Matched MeSH terms: Drug Compounding/methods*
Fulltext Characterization of encapsulated ginger essential oils and its antimicrobial properties

Tengku Shafazila Tengku Saharuddin, Lailatun Nazirah Ozair, Ayuni Shahira Zulkifli, Nursarah Syazwani Hairul Shah, Nur Syafiqah Sahidan

Journal of Academia Universiti Teknologi MARA Negeri Sembilan, 2020;8(1):1-6.
MyJurnal

Ginger essential oils (GEO) are natural products with antibacteria properties consisting of many different volatile
compounds have high potential to be used in many applications. In this study, the ginger GEO was successfully
encapsulated in chitosan as a carrier agent using a spray drying technique. The extraction of Zingiber officinale
(ginger) essential oil is performed by steam distillation method. The GEO was encapsulated in chitosan as a carrier
agents at 1:3, GEO:chitosan ratio by using spray drying technique. GEO together with encapsulated GEO were
further assayed for antimicrobial activity by disc-diffusion method. For characterization of encapsulated GEO,
Fourier transform infrared spectroscopy (FTIR) and Field emission scanning electron microscopy (FESEM) were
used. FTIR analysis revealed that there was no existence of a new functional group in the encapsulated GEO
showing that there is only physical interaction between GEO and chitosan. Besides, FESEM analysis showed the
encapsulated GEO were in micro in sizes and possessed spherical shape with smooth and porous surface.
Furthermore, Both GEO and encapsulated GEO showed in vitro antimicrobial activity against Escheriachia coli,
Pseudomonas aeruginosa, Staphylococcus aureus and Salmonella typhi with encapsulated GEO possessed higher in
the activities for all studied bacteria compared to GEO. The encapsulated GEO demonstrated a superior performance
against Salmonella typhi with the inhibition zone of 22.5 mm compared to GEO only 13.5 mm. The results obtained
indicated that due to the volatility and instability of the GEO when exposed to environmental factors, its encapsulation considerably improve and enhanced its performance.

Matched MeSH terms: Drug Compounding
Fulltext Curcumin Combination Chemotherapy: The Implication and Efficacy in Cancer

Tan BL, Norhaizan ME

Molecules, 2019 Jul 10;24(14).
PMID: 31295906 DOI: 10.3390/molecules24142527

Many chemotherapeutic drugs have been used for the treatment of cancer, for instance, doxorubicin, irinotecan, 5-fluorouracil, cisplatin, and paclitaxel. However, the effectiveness of chemotherapy is limited in cancer therapy due to drug resistance, therapeutic selectivity, and undesirable side effects. The combination of therapies with natural compounds is likely to increase the effectiveness of drug treatment as well as reduce the adverse outcomes. Curcumin, a polyphenolic isolated from Curcuma longa, belongs to the rhizome of Zingiberaceae plants. Studies from in vitro and in vivo revealed that curcumin exerts many pharmacological activities with less toxic effects. The biological mechanisms underlying the anticancer activity of co-treatment curcumin and chemotherapy are complex and worth to discuss further. Therefore, this review aimed to address the molecular mechanisms of combined curcumin and chemotherapy in the treatment of cancer. The anticancer activity of combined nanoformulation of curcumin and chemotherapy was also discussed in this study. Taken together, a better understanding of the implication and underlying mechanisms of action of combined curcumin and chemotherapy may provide a useful approach to combat cancer diseases.

Matched MeSH terms: Drug Compounding
Swelling behaviour and controlled drug release from cross-linked κ-carrageenan/NaCMC hydrogel by diffusion mechanism

Hezaveh H, Muhamad II, Noshadi I, Shu Fen L, Ngadi N

J Microencapsul, 2012;29(4):368-79.
PMID: 22309480 DOI: 10.3109/02652048.2011.651501

We studied a model system of controlled drug release using beta-carotene and κ-carrageenan/NaCMC hydrogel as a drug and a device, respectively. Different concentrations of genipin were added to crosslink the beta-carotene loaded beads by using the dripping method. Results have shown that the cross-linked beads possess lower swelling ability in all pH conditions (pH 1.2 and 7.4), and swelling ratio decreases with increasing genipin concentration. Microstructure study shows that cross-linking has enhanced the stability and structure of the beads network. Determination of diffusion coefficient for the release of encapsulated beta-carotene indicates less diffusivity when beads are cross-linked. Swelling models using adaptive neuro fuzzy show that using genipin as a cross-linker in the kC/NaCMC hydrogels affects the transport mechanism. The model shows very good agreement with the experimental data that indicates that applying ANFIS modelling is an accurate, rapid and simple way to model in such a case for controlled release applications.

Matched MeSH terms: Drug Compounding/methods*
Sodium carboxymethyl cellulose hydrogels containing reduced graphene oxide (rGO) as a functional antibiofilm wound dressing

Ali NH, Amin MCIM, Ng SF

J Biomater Sci Polym Ed, 2019 06;30(8):629-645.
PMID: 30896336 DOI: 10.1080/09205063.2019.1595892

Biofilms comprise bacteria attached to wound surfaces and are major contributors to non-healing wounds. It was found that the increased resistance of biofilms to antibiotics allows wound infections to persist chronically in spite of antibiotic therapy. In this study, the reduced form of graphene oxide (rGO) was explored as plausible antibiofilm agents. The rGO was synthesized via reducing the functional groups of GO. Then, rGO were characterized using zetasizer, X-ray photoelectron spectroscopy, UV-Vis spectroscopy and FESEM. The rGO were then formulated into sodium carboxymethyl cellulose (NaCMC) hydrogels to form rGO hydrogel and tested for antibiofilm activities in vitro using XTT test, and in vivo biofilm formation assay using nematodes C. elegans. Reduced GO hydrogel was successfully formed by reducing the functional groups of GO, and a reduction of up to 95% of functional groups was confirmed with X-ray photoelectron spectroscopy analysis. XTT tests confirmed that rGO hydrogels reduced biofilm formation by S. aureus (81-84%) and P. aeruginosa (50-62%). Fluorescence intensity also confirmed that rGO hydrogel can inhibit biofilm bacteria in C. elegans experiments. This study implied that rGO hydrogel is an effective antibiofilm agent for infected wounds.

Matched MeSH terms: Drug Compounding/methods
In vitro assessment of non-irritant microemulsified voriconazole hydrogel system

Raju Y P, N H, Chowdary V H, Nair RS, Basha D J, N T

Artif Cells Nanomed Biotechnol, 2017 Dec;45(8):1539-1547.
PMID: 27887040 DOI: 10.1080/21691401.2016.1260579

Research was aimed on microemulsion-based hydrogel for voriconazole. Oleic acid and isopropyl myristate as lipid phases; tween 20: tween 80 as surfactants and PEG600 as cosurfactant were selected to formulate voriconazole microemulsions. The promising microemulsions in terms of zeta potential, pH, viscosity, and drug release were selected and developed into hydrogels using carbopol 934. Resulting microemulsion-based hydrogel (MBH) of voriconazole were evaluated for in vitro diffusion and ex vivo permeation. Antifungal potentials of MBH were assessed against selected fungal strains. Optimal MBH formulations, O6 and O8 had displayed their antifungal potentials with enlarged zone of inhibition against selected fungal strains.

Matched MeSH terms: Drug Compounding*
Formulation of Gastric Floating System Using Bio-Sourced Terminalia Catappa Gum and in vivo Evaluation

Meka VS, Murthy Kolapalli VR

Curr Drug Deliv, 2016;13(6):971-81.
PMID: 26452534

A central composite design was applied to design a novel gastric floating drug delivery system comprising propranolol HCl in Terminalia catappa gum and to evaluate the buoyancy, in vitro drug release behavior, and pharmacokinetic parameters. All formulations exhibited good buoyancy properties in vitro reflected by floating lag time of 1-110 sec, total floating time of 9-16 h and prolonged release behaviour (upto 12 h). Statistically optimised formulation (PBGRso) was orally administered to human volunteers under both fasted and fed conditions to evaluate gastric floating behavior under different food conditions by X-ray evaluation. In vivo studies of optimised formulations revealed that the gastric residence time of floating tablets was enhanced in the fed but not in the fasted state. Pharmacokinetic studies of the optimised Terminalia catappa formulation and a commercial product (Ciplar LA 80) carried out on healthy human volunteers showed a significant improvement in the bioavailability (132%) of propranolol HCl released from from the experimental Terminalia catappa formulations compared with Ciplar LA 80.

Matched MeSH terms: Drug Compounding
Development and Standardization of Moringa oleifera Leaves as a Natural Dietary Supplement

Ali MA, Yusof YA, Chin NL, Ibrahim MN, Muneer S

J Diet Suppl, 2019;16(1):66-85.
PMID: 29469600 DOI: 10.1080/19390211.2018.1429517

Moringa oleifera leaves were selected as a model due to their hundreds of health benefits. On the other hand, the powder of these leaves has exhibited poor flowability, low tensile strength, bitter taste, poor dissolution rate, and lack of information regarding dosage. These are the common hurdles and limitations in the adaptation of herbal-based medications. Therefore, a comprehensive study was planned to introduce herbal-based medicines into mainstream medicines by standardization according to the U.S. Food and Drug Administration (FDA) and international pharmaceutical standards. A Simplex Lattice Design (SLD) of Design Expert 8.0 software was used to formulate different concentrations of superdisintegrant, binder/diluent, and sweeteners. An Instron Universal Testing machine coupled with a 13 mm stainless cylindrical die was used to manufacture tablets by means of direct compression method at 20 kN applied force. Therefore, selection of excipients was made on the basis of their tensile strength, flowability, and taste-masking properties. Optimum formulation was tested on rabbits for toxicity and growth rate. All formulated tablets were evaluated on standard parameters for orally disintegrating tablets described by the Food and Drug Authority (U.S.). The optimum formulation fulfills all standard parameters such as hardness, disintegration time, friability, and dissolution rate. The present formulation showed no toxicity when tested on rabbits. The present study provides a fundamental understanding of the tableting characteristics of natural medicines. The present study provides information that will help to overcome the challenges.

Matched MeSH terms: Drug Compounding/methods*
Microencapsulation of alginate-immobilized bagasse with Lactobacillus rhamnosus NRRL 442: enhancement of survivability and thermotolerance

Shaharuddin S, Muhamad II

Carbohydr Polym, 2015 Mar 30;119:173-81.
PMID: 25563958 DOI: 10.1016/j.carbpol.2014.11.045

The aim of this research was to enhance the survivability of Lactobacillus rhamnosus NRRL 442 against heat exposure via a combination of immobilization and microencapsulation processes using sugarcane bagasse (SB) and sodium alginate (NaA), respectively. The microcapsules were synthesized using different alginate concentration of 1, 2 and 3% and NaA:SB ratio of 1:0, 1:1 and 1:1.5. This beneficial step of probiotic immobilization before microencapsulation significantly enhanced microencapsulation efficiency and cell survivability after heat exposure of 90°C for 30s. Interestingly, the microcapsule of SB-immobilized probiotic could obtain protection from heat using microencapsulation of NaA concentration as low as 1%. SEM images illustrated the incorporation of immobilized L. rhamnosus within alginate matrices and its changes after heat exposure. FTIR spectra confirmed the change in functional bonding in the presence of sugarcane bagasse, probiotic and alginate. The results demonstrated a great potential in the synthesis of heat resistant microcapsules for probiotic.

Matched MeSH terms: Drug Compounding/methods*
Influence of beta-cyclodextrin and chitosan in the formulation of a colon-specific drug delivery system

Rehman K, Amin MC, Muda S

Drug Res (Stuttg), 2013 Dec;63(12):657-62.
PMID: 23842943 DOI: 10.1055/s-0033-1349129

The increase in diseases of the colon underscores the need to develop cost-effective site-directed therapies. We formulated a polysaccharide-based matrix system that could release ibuprofen under conditions simulating those in the colon by employing a wet granulation method. Tablets were prepared in a series of formulations containing a polysaccharide (beta-cyclodextrin and chitosan) matrix system along with ethylcellulose. We characterized physicochemical properties and performed an in vitro drug release assay in the absence and presence of digestive enzymes to assess the ability of the polysaccharides to function as a protective barrier against the upper gastrointestinal environment. Fourier transform infrared spectroscopy studies revealed no chemical interaction between ibuprofen and polysaccharides; however, spectrum analysis suggested the formation of an inclusion complex of beta-cyclodextrin with ibuprofen. The formulations contained 50% ethylcellulose and 50% beta-cyclodextrins (1:1) were proven to be the better formulation that slowly released the drug until 24 h (101.04 ± 0.65% maximum drug release in which 83.08 ± 0.89% drug was released in colonic medium) showed better drug release profiles than the formulations containing chitosan. We conclude that a beta-cyclodextrin drug carrier system may represent an effective approach for treatment of diseases of the colon.

Matched MeSH terms: Drug Compounding/methods
Exploring role of polysaccharides present in Ganoderma lucidium extract powder and probiotics as solid carriers in development of liquisolid formulation loaded with quercetin: A novel study

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
Fulltext Nanoparticle-Encapsulated Camptothecin: Epigenetic Modulation in DNA Repair Mechanisms in Colon Cancer Cells

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

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