Colon-targeting of progesterone using hybrid polymeric microspheres improves its bioavailability and in vivo biological efficacy

Gadalla, Hytham H.; Mohammed, F. A.; El‐Sayed, Ahmed M.; Soliman, Ghareb M.

doi:10.1016/j.ijpharm.2020.119070

Cited by 21 publications

(8 citation statements)

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“…Ionotropicaly cross-linked alginate polymer matrices were pH-responsive [ 75 ]. The swelling index was significantly lower in pH 1.2 buffers, and microspheres were stable in an acidic medium, as reported earlier ( Figure 6 a) [ 76 , 77 ]. Lower swelling and stability of PAG-alginate microspheres in an acidic environment are most likely due to the replacement of protons with calcium ions to form insoluble alginic acid pursued by solvent penetration [ 78 ].…”

Section: Resultssupporting

confidence: 86%

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Prunus armeniaca Gum-Alginate Polymeric Microspheres to Enhance the Bioavailability of Tramadol Hydrochloride: Formulation and Evaluation

et al. 2022

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Combinations of polymers can improve the functional properties of microspheres to achieve desired therapeutic goals. Hence, the present study aimed to formulate Prunus armeniaca gum (PAG) and sodium alginate microsphere for sustained drug release. Blended and coated microspheres were prepared using the ionotropic gelation technique. The effect of polymer concentration variation was studied on the structural and functional properties of formulated microspheres. FTIR, XRD, and thermal analysis were performed to characterize the microspheres. All the formulations were well-formed spherical beads having an average diameter from 579.23 ± 07.09 to 657.67 ± 08.74 μm. Microspheres entrapped drugs within the range 65.86 ± 0.26–83.74 ± 0.79%. The pH-dependent swelling index of coated formulations was higher than blended. FTIR spectra confirmed the presence of characteristic peaks of entrapped Tramadol hydrochloride showing no drug-polymer interaction. In vitro drug release profile showed sustained release following the Korsmeyer-Peppas kinetic model with an R2 value of 0.9803–0.9966. An acute toxicology study employing the oral route in Swiss albino mice showed no signs of toxicity. It can be inferred from these results that blending PAG with sodium alginate can enhance the stability of alginate microspheres and improve its drug release profile by prolonging the release time.

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Section: Resultssupporting

confidence: 86%

“…In pH 7.4, all types of microspheres showed significantly higher swelling ( Figure 6 b). This was due to the relaxation of polymeric chains and deprotonation of carboxylic acid groups in the basic medium [ 77 , 79 ]. In 7.4 pH alginate microspheres, TA-1 showed maximum swelling up to 6 h and started to disintegrate [ 16 ].…”

Section: Resultsmentioning

confidence: 99%

Prunus armeniaca Gum-Alginate Polymeric Microspheres to Enhance the Bioavailability of Tramadol Hydrochloride: Formulation and Evaluation

et al. 2022

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“…Xiong et al [ 168 ] showed that encapsulation of resveratrol in ovalbumin-CMC nanoparticles increased the bioaccessibility of resveratrol to 80%, demonstrating an improvement from native resveratrol. Gadalla et al [ 169 ] used pectin-NaCMC microspheres to deliver progesterone to the colon, and found a 1.8-fold increase in AUC and 2.3-fold increase in mean residence time when compared to a free solution of progesterone. Kaur et al [ 170 ] developed EC nanoparticles for amphotericin B delivery for antifungal applications, and demonstrated a 15-fold improvement in oral bioavailability when compared to a free solution of amphotericin B.…”

Section: Mucoadhesive Drug Delivery Systemsmentioning

confidence: 99%

Mucus interaction to improve gastrointestinal retention and pharmacokinetics of orally administered nano-drug delivery systems

2022

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Oral delivery of therapeutics is the preferred route of administration due to ease of administration which is associated with greater patient medication adherence. One major barrier to oral delivery and intestinal absorption is rapid clearance of the drug and the drug delivery system from the gastrointestinal (GI) tract. To address this issue, researchers have investigated using GI mucus to help maximize the pharmacokinetics of the therapeutic; while mucus can act as a barrier to effective oral delivery, it can also be used as an anchoring mechanism to improve intestinal residence. Nano-drug delivery systems that use materials which can interact with the mucus layers in the GI tract can enable longer residence time, improving the efficacy of oral drug delivery. This review examines the properties and function of mucus in the GI tract, as well as diseases that alter mucus. Three broad classes of mucus-interacting systems are discussed: mucoadhesive, mucus-penetrating, and mucolytic drug delivery systems. For each class of system, the basis for mucus interaction is presented, and examples of materials that inform the development of these systems are discussed and reviewed. Finally, a list of FDA-approved mucoadhesive, mucus-penetrating, and mucolytic drug delivery systems is reviewed. In summary, this review highlights the progress made in developing mucus-interacting systems, both at a research-scale and commercial-scale level, and describes the theoretical basis for each type of system.

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“…Over the years, several studies reported adhesion of drug carrier systems to gastrointestinal mucosa to allow greater residence time and release of the drug payload . The carrier systems included nanoparticles (NPs) self-emulsifying systems, hydrogels, polymeric patches, iontophoretic patches, and microneedle patches. − These studies aimed to improve the residence time and allow the controlled release of therapeutics to enhance systemic absorption and bioavailability . In general, the drug carriers are made of polymers that would interact with the mucosal layer by physical entanglement, electrostatic attraction, and van der Waal’s forces to facilitate adhesion .…”

Section: Introductionmentioning

confidence: 99%

Functionalized LbL Film for Localized Delivery of STAT3 siRNA and Oxaliplatin Combination to Treat Colon Cancer

Janardhanam

Bandi

Venuganti

2022

ACS Appl. Mater. Interfaces

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The aim of the study was to develop and evaluate the efficacy of a functionalized layer-by-layer (LbL) assembled film entrapped with oxaliplatin (OX) and signal transducer and activator of transcription 3 (STAT3) siRNA in the localized treatment of colon cancer. The LbL film was prepared by the sequential layering of chitosan (CS) and alginate to attain desired physical and mechanical properties. The film was functionalized by coating folic acid-conjugated CS on one side. On the other side, polycaprolactone was coated as a backing layer to provide directional drug release. OX was entrapped within the layers of the film, while STAT3 siRNA was complexed with CS to form nanoparticles before entrapment in the LbL film. The CS–siRNA nanoparticles were taken up by the colon carcinoma, Caco-2 cells within 3 h and provided concentration-dependent reduction in STAT3 protein expression. The functionalized LbL film (F-LbL film) selectively adhered to the colon cancer tissue in the mice model, whereas the nonfunctionalized film adhered to the normal colon tissue. The combination of OX and STAT3 siRNA provided significantly greater tumor regression, survival rate, and STAT3 protein suppression after localized delivery through oral administration compared with intravenous administration. Taken together, the F-LbL film can selectively bind to colon tumors for localized delivery of drugs to treat colon cancer.

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Colon-targeting of progesterone using hybrid polymeric microspheres improves its bioavailability and in vivo biological efficacy

Cited by 21 publications

References 50 publications

Prunus armeniaca Gum-Alginate Polymeric Microspheres to Enhance the Bioavailability of Tramadol Hydrochloride: Formulation and Evaluation

Prunus armeniaca Gum-Alginate Polymeric Microspheres to Enhance the Bioavailability of Tramadol Hydrochloride: Formulation and Evaluation

Mucus interaction to improve gastrointestinal retention and pharmacokinetics of orally administered nano-drug delivery systems

Functionalized LbL Film for Localized Delivery of STAT3 siRNA and Oxaliplatin Combination to Treat Colon Cancer

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