Enhancement of Bioavailability Through Transdermal Drug Delivery of Paliperidone Palmitate-Loaded Nanostructured Lipid Carriers

Raval, Shilpa; Jani, Parva; Patil, Pravin; Thakkar, Parth; Sawant, Krutika

doi:10.4155/tde-2021-0036

Cited by 4 publications

(3 citation statements)

References 59 publications

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“…Thus, PPD was approved for an extended-release (ER) tablet (Invega ® , Janssen, Antwerp, Belgium) for a once-daily administration based on an osmotic-controlled release oral Push–Pull™ delivery system (Oral Osmotic System, OROS ® , Alza Corporation, Mountain View, CA, USA) [ 6 ]. In addition, studies on liquid suspensions using ion exchange resin, oral formulation using lipid nanostructures, and injections using liposome systems have been conducted for the controlled release of PPD [ 7 , 8 , 9 ].…”

Section: Introductionmentioning

confidence: 99%

Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release

et al. 2023

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This study aimed to develop electrolyte complexes of paliperidone (PPD) with various particle sizes using cation-exchange resins (CERs) to enable controlled release (both immediate and sustained release). CERs of specific particle size ranges were obtained by sieving commercial products. PPD–CER complexes (PCCs) were prepared in an acidic solution of pH 1.2 and demonstrated a high binding efficiency (>99.0%). PCCs were prepared with CERs of various particle sizes (on average, 100, 150, and 400 μm) at the weight ratio of PPD to CER (1:2 and 1:4). Physicochemical characterization studies such as Fourier-transform infrared spectroscopy, differential scanning calorimetry, powder X-ray diffraction, and scanning electron microscopy between PCCs (1:4) and physical mixtures confirmed PCC formation. In the drug release test, PPD alone experienced a complete drug release from PCC of >85% within 60 min and 120 min in pH 1.2 and pH 6.8 buffer solutions, respectively. Alternatively, PCC (1:4) prepared with CER (150 μm) formed spherical particles and showed an almost negligible release of PPD in pH 1.2 buffer (<10%, 2 h) while controlling the release in pH 6.8 buffer (>75%, 24 h). The release rate of PPD from PCCs was reduced with the increase in CER particle size and CER ratio. The PCCs explored in this study could be a promising technology for controlling the release of PPD in a variety of methods.

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Section: Introductionmentioning

confidence: 99%

Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release

et al. 2023

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“…Formulation techniques such as cocrystallization [10], lipid nanoconstructs [8], and ion-exchange resin complexes [11] were attempted. Similarly, transdermal and nose-to-brain routes were also assessed [4,9,12,13].…”

Section: Introductionmentioning

confidence: 99%

Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers

AlMulhim,

Nair,

Aldhubiab

et al. 2023

Pharmaceutics

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The therapeutic effectiveness of paliperidone in the treatment of schizophrenia has been limited by its poor oral bioavailability; hence, an alternative route could be appropriate. This study investigates the feasibility of developing a buccal film impregnated with paliperidone-loaded nanostructured lipid carriers (NLCs) and assesses the potential to enhance its bioavailability. Box–Behnken-based design optimization of NLCs was performed by examining the particles’ physical characteristics. The polymeric film was used to load optimized NLCs, which were then assessed for their pharmaceutical properties, permeability, and pharmacokinetics. The optimization outcomes indicated that selected formulation variables had a considerable (p < 0.05) impact on responses such as particle size, entrapment efficiency, and % drug release. Desired characteristics such as a negative charge, higher entrapment efficiency, and nanoparticles with ideal size distribution were shown by optimized NLC dispersions. The developed film demonstrated excellent physico-mechanical properties, appropriate texture, good drug excipient compatibility (chemically stable formulation), and amorphous drug nature. A sustained Weibull model drug release (p < 0.0005) and superior flux (~5-fold higher, p < 0.005) were seen in NLC-loaded film compared to plain-drug-loaded film. The pharmacokinetics profile in rabbits supports the goal of buccal therapy as evidenced by significantly higher AUC0–12 (p < 0.0001) and greater relative bioavailability (236%) than the control. These results support the conclusion that paliperidone-loaded NLC buccal film has the potential to be an alternate therapy for its effective administration in the treatment of schizophrenia.

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“…Comparing the stratum corneum to the other epithelial barriers of the gastrointestinal, rectal, nasal, buccal and vaginal pathways, the stratum corneum is the supreme terrifying barrier because of its peculiar composition (proteins: lipids: water = 40:40:20%, respectively) and tight intercellular connections. Drugs are applied topically either for local or systemic effects, depending on their intended use [7].…”

Section: Introductionmentioning

confidence: 99%

Niosomes a Promissing Nanocarrier: A Review

BHANGE,

PETHE,

JADHAV

2023

Int J App Pharm

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There are numerous traditional methods for applying medications to the skin. Transdermal has become a popular method of drug delivery in recent years for a variety of medications that are difficult to administer in other ways. Transdermal drug delivery has a number of advantages, the most important of which is the prevention of first-pass metabolism and the stomach environment, which would render the drug inactive. In addition to discussing in depth the various formulation techniques and permeability enhancement for improved therapeutic efficacy, a transdermal patch allows for the controlled release of medication into the patient, typically through membrane pores that house a reserve of medication or over body heat that melts thin layers of medication entrenched in the adhesive. The drug molecules can permeate the skin and be administered in this manner. Niosomes are vesicles made of non-ionic surfactants that are more stable, biodegradable, and generally harmless. Because surfactants are more chemically stable than lipids, niosomes are ideal for liposomes. The main topics of this review study are the concept of niosome, its benefits and drawbacks, composition, various type of transdermal formulation, enhancers using in this delivery and novel transdermal drug delivery, variables influencing niosomes, characterization, and use of noisome. Niosomes can be used to carry both amphiphilic and lipophilic drugs. Niosomes have great potential in targeted drug delivery of anticancer and anti-infective agents. This review article represents the structure of Niosomes, its advantages and disadvantages, types of niosomes, applications, method of preparation of niosomes.

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Enhancement of Bioavailability Through Transdermal Drug Delivery of Paliperidone Palmitate-Loaded Nanostructured Lipid Carriers

Cited by 4 publications

References 59 publications

Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release

Paliperidone–Cation Exchange Resin Complexes of Different Particle Sizes for Controlled Release

Design, Development, Evaluation, and In Vivo Performance of Buccal Films Embedded with Paliperidone-Loaded Nanostructured Lipid Carriers

Niosomes a Promissing Nanocarrier: A Review

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