Sulpiride (Su), belonging to the benzamine class, is an antipsychotic medication utilized for the treatment of several psychotic diseases [ 1 ]. Psychotic disorders afflict 1% of the general population, with a high prevalence (16%) among those with a family history of schizophrenia [ 2 ]. Sulpiride is an antipsychotic medication that selectively blocks central dopamine receptors [ 3 ]. Su has garnered significant attention among many anti-psychotic medications due to its non-toxic nature, fewer extrapyramidal side effects, decreased affinity for other neural receptors, and cost-effectiveness [ 4 ]. However, Su has a number of challenges that need to be overcome. It is categorized as a class IV drug in the biopharmaceutical classification system. Consequently, Su has low solubility in water and restricted permeability through the intestines [ 5 ]. Therefore, a previously reported poor oral bioavailability (20&#;30%) has been demonstrated [ 6 ]. Moreover, the administration of large amounts of the medication is necessary to treat patients, leading to troublesome adverse reactions such as cardiovascular effects, sleep problems, agitation, over-stimulation and minor extrapyramidal effects [ 7 ]. Furthermore, Su exhibits an absorption window in the upper gastrointestinal tract [ 8 ]. These factors contribute to the observed low effectiveness of the drug when taken orally and its unpredictable absorption into the bloodstream through the digestive system. Therefore, there is an increasing demand for the development of approaches to improve its characteristics. Several strategies have been employed to address the challenges of the oral administration of Sulpiride. These strategies include the use of solid lipid nanoparticles [ 7 ], self-micro-emulsifying carriers [ 9 ], and solid dispersions [ 10 ]. However, the outcomes of these attempts have been limited because they have focused on the problem of Sulpiride&#;s poor aqueous solubility. Therefore, other platforms are required to address other routes of administration, such as transdermal application, to improve the pharmacological effectiveness of the drug.
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Transdermal drug delivery (TDD) is currently an area of considerable interest for both researchers and pharmaceutical manufacturers. Transdermal drug delivery has become a feasible substitute for oral administration for systemic drug delivery. Transdermal medication delivery is becoming more popular due to its many benefits compared to oral administration. From a therapeutic point of view, it mitigates variations in the levels of medicines in the bloodstream, particularly for medications with a short half-life. In addition, the enhanced bioavailability resulting from the avoidance of first-pass metabolism allows for the administration of lower dosages to achieve the desired bioavailability. Transdermal drug delivery (TDD) enables prolonged drug release by circumventing issues related to drug absorption following oral administration, such as the pH and activity of enzymes [ 11 ]. This, in turn, reduces the systemic adverse effects and enhances the safety margin of the administered drugs [ 12 ]. The convenience and patient-friendly nature of transdermal drug delivery (TDD) is attributed to aspects such as reduced dose frequency, non-invasive administration and ease of application [ 13 ]. These factors contribute to improved patient adherence, particularly in cases of extended periods of treatment, such as in the management of chronic pain [ 14 ]. Therefore, the transdermal administration of antipsychotic drugs is a dependable approach to boost medication adherence and reduce the need for numerous doses, hence improving patient compliance. However, the most superficial layer of the skin (stratum corneum) acts as an obstacle, preventing drugs from being absorbed systemically. As a result, it may restrict the amount of drugs that can be absorbed into the bloodstream when administered through the skin [ 15 ]. El-Tokhy et al. concluded that the transdermal delivery of antipsychotics demonstrated improved therapeutic outcomes compared to oral administration [ 16 ]. However, formulations based on nanotechnology have provided several benefits and greater effectiveness compared to traditional methods. Moreover, systems based on phospholipids are highly recommended for the delivery of antipsychotics, and the lipid core effectively dissolves lipophilic compounds, resulting in a high percentage of drug loading. Alnaim et al. suggested that the use of niosomal gel formulation loaded with levosulpiride, administered transdermally, could enhance the effectiveness of the drug and may serve as a viable alternative to traditional therapy [ 17 ].
18,Recent studies have highlighted the potential application of nano-vesicular formulations as carriers that can improve the penetration of hydrophobic and/or hydrophilic medicines via the skin. This has been supported by several studies [ 15 19 ]. Phospholipid-based nano-vesicular carriers have shown effectiveness in reducing the lipid barrier of the skin [ 20 ], facilitating the permeation of drugs into the skin&#;s deeper layers and their absorption into the systemic circulation. Bilosomes are phospholipid- and bile-salt-based deformable and flexible lipid vesicles that exhibit significant advantages over traditional vesicles (liposomes and niosomes) with respect to high stability and a simplified manufacturing process [ 21 ]. Bilosomes serve as a drug delivery system, and have several benefits including high biocompatibility and biodegradability with little toxicity, self-assembly capability, easy removal from the body, and an enhanced effectiveness and bioavailability of enclosed substances. Therefore, the use of a biocompatible bile salt, namely sodium deoxycholate (SDC), could enhance the stability of bilosomes and exceed the stability of conventional liposomes. Bile salts are a kind of bio-surfactant that enhance the bioavailability of drugs in the presence of obstacles for absorption, such as limited permeability across cell membranes or poor solubility in water [ 22 ]. In addition, bile salts greatly reduce the temperature at which lipids undergo phase transition, resulting in bilosomal vesicles that are extremely deformable and flexible at physiological temperature. The flexibility of bilosomal vesicles greatly facilitates transdermal application through enhancing penetration into the skin&#;s deep layers [ 23 ]. Significantly, the presence of bile salts, sodium deoxycholate (SDC), greatly improves the stability of bilosomal vesicles, in comparison to other traditional vesicles [ 24 ]. As a result, bilosomes have been used in numerous investigations to improve the transdermal administration of various medications, including niflumic acid [ 25 ], tizanidine hydrochloride [ 26 ], and lornoxicam [ 27 ].
Bilosomal gels are polymer networks that have a three-dimensional structure and are capable of absorbing significant amounts of biological fluids or water. Due to their distinctive physical characteristics, including as biocompatibility, flexibility, biodegradability, high porosity, and controlled drug release, they are intriguing tools for drug delivery applications [ 28 ].
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Currently, there are no recorded studies that have evaluated the possibility of bilosomes as carriers for delivering Sulpiride. Consequently, the main objective of the current study was to use nanovesicles along with in vitro and in vivo studies to find an innovative approach for antipsychotic medications. In addition, our goal was to design appropriate nano-vesicles for transdermal administration to ameliorate the in vivo performance of Sulpiride encapsulated in bilosomes.
In this study, we created and examined a bilosomal delivery system containing Sulpiride (Su) to assess its bioavailability after being applied to the skin. Sulpiride-loaded bilosomes were created, utilizing thin film hydration technique. The Box&#;Behnken design (BBD) was used to optimize the bilosomal vesicles. Subsequently, the bilosomes that were optimized underwent characterization to determine their particle size, morphology, and entrapment efficiency. In our study, the in vitro drug release, ex vivo drug permeation, and pharmacokinetics activity of Su-loaded bilosomal gel were evaluated and compared with those of free drug and Sulpiride-loaded gel.
Future prospects for the emerging promising nano-vesicular systems could involve more examinations of bilosomal fate and the use of advanced technology for targeting, as this delivery method has not yet been fully explored. Additional investigations, including in vivo and preclinical studies, should be taken in consideration in order to prepare such delivery systems for competition in the pharmaceutical industry.
Sulpiride (Su), belonging to the benzamine class, is an antipsychotic medication utilized for the treatment of several psychotic diseases [ 1 ]. Psychotic disorders afflict 1% of the general population, with a high prevalence (16%) among those with a family history of schizophrenia [ 2 ]. Sulpiride is an antipsychotic medication that selectively blocks central dopamine receptors [ 3 ]. Su has garnered significant attention among many anti-psychotic medications due to its non-toxic nature, fewer extrapyramidal side effects, decreased affinity for other neural receptors, and cost-effectiveness [ 4 ]. However, Su has a number of challenges that need to be overcome. It is categorized as a class IV drug in the biopharmaceutical classification system. Consequently, Su has low solubility in water and restricted permeability through the intestines [ 5 ]. Therefore, a previously reported poor oral bioavailability (20&#;30%) has been demonstrated [ 6 ]. Moreover, the administration of large amounts of the medication is necessary to treat patients, leading to troublesome adverse reactions such as cardiovascular effects, sleep problems, agitation, over-stimulation and minor extrapyramidal effects [ 7 ]. Furthermore, Su exhibits an absorption window in the upper gastrointestinal tract [ 8 ]. These factors contribute to the observed low effectiveness of the drug when taken orally and its unpredictable absorption into the bloodstream through the digestive system. Therefore, there is an increasing demand for the development of approaches to improve its characteristics. Several strategies have been employed to address the challenges of the oral administration of Sulpiride. These strategies include the use of solid lipid nanoparticles [ 7 ], self-micro-emulsifying carriers [ 9 ], and solid dispersions [ 10 ]. However, the outcomes of these attempts have been limited because they have focused on the problem of Sulpiride&#;s poor aqueous solubility. Therefore, other platforms are required to address other routes of administration, such as transdermal application, to improve the pharmacological effectiveness of the drug.
Transdermal drug delivery (TDD) is currently an area of considerable interest for both researchers and pharmaceutical manufacturers. Transdermal drug delivery has become a feasible substitute for oral administration for systemic drug delivery. Transdermal medication delivery is becoming more popular due to its many benefits compared to oral administration. From a therapeutic point of view, it mitigates variations in the levels of medicines in the bloodstream, particularly for medications with a short half-life. In addition, the enhanced bioavailability resulting from the avoidance of first-pass metabolism allows for the administration of lower dosages to achieve the desired bioavailability. Transdermal drug delivery (TDD) enables prolonged drug release by circumventing issues related to drug absorption following oral administration, such as the pH and activity of enzymes [ 11 ]. This, in turn, reduces the systemic adverse effects and enhances the safety margin of the administered drugs [ 12 ]. The convenience and patient-friendly nature of transdermal drug delivery (TDD) is attributed to aspects such as reduced dose frequency, non-invasive administration and ease of application [ 13 ]. These factors contribute to improved patient adherence, particularly in cases of extended periods of treatment, such as in the management of chronic pain [ 14 ]. Therefore, the transdermal administration of antipsychotic drugs is a dependable approach to boost medication adherence and reduce the need for numerous doses, hence improving patient compliance. However, the most superficial layer of the skin (stratum corneum) acts as an obstacle, preventing drugs from being absorbed systemically. As a result, it may restrict the amount of drugs that can be absorbed into the bloodstream when administered through the skin [ 15 ]. El-Tokhy et al. concluded that the transdermal delivery of antipsychotics demonstrated improved therapeutic outcomes compared to oral administration [ 16 ]. However, formulations based on nanotechnology have provided several benefits and greater effectiveness compared to traditional methods. Moreover, systems based on phospholipids are highly recommended for the delivery of antipsychotics, and the lipid core effectively dissolves lipophilic compounds, resulting in a high percentage of drug loading. Alnaim et al. suggested that the use of niosomal gel formulation loaded with levosulpiride, administered transdermally, could enhance the effectiveness of the drug and may serve as a viable alternative to traditional therapy [ 17 ].
18,Recent studies have highlighted the potential application of nano-vesicular formulations as carriers that can improve the penetration of hydrophobic and/or hydrophilic medicines via the skin. This has been supported by several studies [ 15 19 ]. Phospholipid-based nano-vesicular carriers have shown effectiveness in reducing the lipid barrier of the skin [ 20 ], facilitating the permeation of drugs into the skin&#;s deeper layers and their absorption into the systemic circulation. Bilosomes are phospholipid- and bile-salt-based deformable and flexible lipid vesicles that exhibit significant advantages over traditional vesicles (liposomes and niosomes) with respect to high stability and a simplified manufacturing process [ 21 ]. Bilosomes serve as a drug delivery system, and have several benefits including high biocompatibility and biodegradability with little toxicity, self-assembly capability, easy removal from the body, and an enhanced effectiveness and bioavailability of enclosed substances. Therefore, the use of a biocompatible bile salt, namely sodium deoxycholate (SDC), could enhance the stability of bilosomes and exceed the stability of conventional liposomes. Bile salts are a kind of bio-surfactant that enhance the bioavailability of drugs in the presence of obstacles for absorption, such as limited permeability across cell membranes or poor solubility in water [ 22 ]. In addition, bile salts greatly reduce the temperature at which lipids undergo phase transition, resulting in bilosomal vesicles that are extremely deformable and flexible at physiological temperature. The flexibility of bilosomal vesicles greatly facilitates transdermal application through enhancing penetration into the skin&#;s deep layers [ 23 ]. Significantly, the presence of bile salts, sodium deoxycholate (SDC), greatly improves the stability of bilosomal vesicles, in comparison to other traditional vesicles [ 24 ]. As a result, bilosomes have been used in numerous investigations to improve the transdermal administration of various medications, including niflumic acid [ 25 ], tizanidine hydrochloride [ 26 ], and lornoxicam [ 27 ].
Bilosomal gels are polymer networks that have a three-dimensional structure and are capable of absorbing significant amounts of biological fluids or water. Due to their distinctive physical characteristics, including as biocompatibility, flexibility, biodegradability, high porosity, and controlled drug release, they are intriguing tools for drug delivery applications [ 28 ].
Currently, there are no recorded studies that have evaluated the possibility of bilosomes as carriers for delivering Sulpiride. Consequently, the main objective of the current study was to use nanovesicles along with in vitro and in vivo studies to find an innovative approach for antipsychotic medications. In addition, our goal was to design appropriate nano-vesicles for transdermal administration to ameliorate the in vivo performance of Sulpiride encapsulated in bilosomes.
In this study, we created and examined a bilosomal delivery system containing Sulpiride (Su) to assess its bioavailability after being applied to the skin. Sulpiride-loaded bilosomes were created, utilizing thin film hydration technique. The Box&#;Behnken design (BBD) was used to optimize the bilosomal vesicles. Subsequently, the bilosomes that were optimized underwent characterization to determine their particle size, morphology, and entrapment efficiency. In our study, the in vitro drug release, ex vivo drug permeation, and pharmacokinetics activity of Su-loaded bilosomal gel were evaluated and compared with those of free drug and Sulpiride-loaded gel.
Future prospects for the emerging promising nano-vesicular systems could involve more examinations of bilosomal fate and the use of advanced technology for targeting, as this delivery method has not yet been fully explored. Additional investigations, including in vivo and preclinical studies, should be taken in consideration in order to prepare such delivery systems for competition in the pharmaceutical industry.